Home Immunology & Inflammation IL Receptor modulator - Glucocorticoid Receptor inhibitor - Mitophagy activator - Autophagy activator - COVID-19 inhibitor - Complement System inhibitor Dexamethasone For research use only.

Dexamethasone

Synonyms: NSC 34521, Hexadecadrol, Prednisolone F,MK-125

Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients.

Dexamethasone Chemical Structure

Dexamethasone Chemical Structure

CAS: 50-02-2

Selleck's Dexamethasone has been cited by 100 publications

Purity & Quality Control

Batch: Purity: 99.68%
99.68

Products often used together with Dexamethasone

Pomalidomide

Dexamethasone and Pomalidomide application in treating relapsed or refractory multiple myeloma is still under clinical trials.

Siegel DS, et al. Br J Haematol. 2020;188(4):501-510.

Bortezomib

Dexamethasone and Bortezomib use results in highly effective and well-tolerated regimen for frontline treatment of multiple myeloma (MM).

Hassan Zafar MS, et al. South Asian J Cancer. 2018;7(1):58-60.

Venetoclax (ABT-199)

Dexamethasone and Venetoclax combination therapy induces long-term leukemia-free survival in PDX models.

Kirchhoff H, et al. Blood. 2021;137(19):2657-2661.

Lenalidomide

Dexamethasone and Lenalidomide demonstrate potent anti-MM activities both in vitro and in randomized phase III clinical trials.

Hideshima T, et al. Ther Clin Risk Manag. 2008;4(1):129-136.

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human monocytes Function assay 5 μM 20 h Antiinflammatory activity in human monocytes assessed as inhibition of LPS-induced COX2 expression at 5 uM after 20 hrs using rabbit polyclonal antibody IgG by SDS-PAGE analysis 21843935
rat polymorphonuclear leukocytes Function assay 20 mins Antiinflammatory activity in rat polymorphonuclear leukocytes assessed as inhibition of LPS-stimulated nitric oxide production after 20 mins by Griess method, IC50=2.3 nM 22506620
mouse thymocytes Function assay 1 μM 24 h Induction of apoptosis in mouse thymocytes assessed as internucleosomal DNA fragmentation at 1 uM after 24 hrs by agarose gel electrophoresis 24794748
T-cell Function assay Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells, IC50 = 0.005 μM. 11229767
PBMC Function assay Inhibitory concentration against TNF-alpha production from human peripheral blood mononuclear cells stimulated by LPS, IC50 = 0.01 μM. 11229767
PBMC Function assay Inhibitory concentration against growth of LPS stimulated human peripheral blood mononuclear cells, IC50 = 0.04 μM. 11229767
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as effect on TNFalpha formation pretreated 1 hr before LPS challenge measured after 24 hrs, IC50 = 0.7 μM. 11908984
N9 Function assay Inhibitory activity against TNF-alpha release in N9 cells in the supernatant, IC50 = 0.074 μM. 12361395
RAW 264.7 Function assay Inhibitory activity against TNF-alpha release in RAW 264.7 cells in the supernatant, IC50 = 0.42 μM. 12361395
A549 Function assay 10 uM Antagonist activity for Glucocorticoid receptor in MMTV transactivation assay in human A549 lung epithelial cells at 10 uM, IC50 = 10 μM. 15999989
A549 Function assay Activity at glucocorticoid receptor in human A549 cells assessed as effect on GRE promoter response by luciferase reporter assay, EC50 = 0.001 μM. 16643060
A549 Function assay Agonist activity at GR assessed as MMTV-mediated transactivation of renilla luciferase gene in human A549 cells relative to Dexamethasone, EC50 = 0.005012 μM. 16821781
A549 Function assay Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cells, IC50 = 0.001175 μM. 16821781
HFF Function assay Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay, EC50 = 0.0019 μM. 17181172
HeLa Function assay Activation of MMTV in HeLa cells measured by luciferase activity, EC50 = 0.017 μM. 17181172
HFF Function assay Inhibition of IL1-stimulated IL6 production in HFF cells, IC50 = 0.00051 μM. 17181172
RAW 264.7 Function assay 24 hrs Inhibition of interferon gamma-stimulated NO production in RAW 264.7 cells after 24 hrs, IC50 = 0.02 μM. 17367124
RAW264.7 Function assay 2 hrs Inhibition of COX2 expression in LPS-stimulated mouse RAW264.7 cells after 2 hrs by Western blot analysis 17407277
RAW264.7 Function assay 2 hrs Inhibition of mPGES1 expression in LPS-stimulated mouse RAW264.7 cells after 2 hrs by Western blot analysis 17407277
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay, EC50 = 0.00537 μM. 17616395
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM. 17616395
A549 Function assay Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation, IC50 = 1 μM. 17616395
HFF Antiinflammatory assay Antiinflammatory activity assessed as inhibition of IL1 stimulated IL6 production in HFF cells by transrepression assay, EC50 = 0.0005 μM. 17692519
HFF Antiinflammatory assay Antiinflammatory activity assessed as upregulation of aromatase in HFF cells by transactivation assay, EC50 = 0.002 μM. 17692519
CV1 Function assay Agonist activity at human GR expressed in CV1 cells by GRE activation assay, EC50 = 0.0002 μM. 17705362
NHDFneo Function assay Activity at human GR expressed in NHDFneo cells assessed as inhibition of IL-6 production, IC50 = 0.0014 μM. 17705362
RPMI8226 Antiproliferative assay 4 days Antiproliferative activity against human RPMI8226 cells after 4 days, IC50 = 0.0065 μM. 17705362
J774A.1 Function assay Inhibition of LPS-induced TNFalpha production in mouse J774A.1 cells, IC50 = 0.048 μM. 17892941
CV1 Function assay Activity at human glucocorticoid receptor expressed in CV1 cells assessed as repression of TNF and IL-1-beta-induced E-selectin gene expression by luciferase reporter gene assay, ED50 = 0.0001 μM. 18032610
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay, EC50 = 0.005012 μM. 18038970
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001175 μM. 18038970
COS7 Function assay 1 uM Agonist activity at glucocorticoid receptor Q570A mutant in COS7 cells at 1 uM by NF-kappaB-luciferase reporter gene assay 18038970
HeLa Cytotoxicity assay Cytotoxicity against human HeLa cells assessed as inhibition of DNA replication by imaging analysis 18066055
HeLa Function assay Inhibition of mitosis in human HeLa cells by imaging analysis 18066055
R1 Function assay 10 uM 24 hrs Inhibition of glucocorticoid receptor-glucocorticoid complex transfected in rat R1 cells assessed as down-regulation of TPA-responsive element proinflammatory gene expression at 10 uM after 24 hrs by beta-galactosidase assay, IC50 = 0.005 μM. 18412397
THP1 Antiinflammatory assay Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 by ELISA, IC50 = 0.007 μM. 18625560
THP1 Antiinflammatory assay Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha by ELISA, IC50 = 0.05 μM. 18625560
RAW264.7 Function assay 10 uM Inhibition of LPS-stimulated COX2 expression in mouse RAW264.7 cells at 10 uM by Western blot 18790649
RAW264.7 Function assay Inhibition of LPS-stimulated microsomal prostaglandin E synthase 1 expression at 10 uM in mouse RAW264.7 cells by Western blot 18790649
A549 Function assay Transrepression activity at GR in IL-1-beta-stimulated human A549 cells assessed as inhibition of NF-kappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM. 19321341
A549 Function assay Transrepression activity at GR in PMA-stimulated human A549 cells assessed as inhibition of AP1 response element-induced luciferase reporter gene activity, EC50 = 0.0025 μM. 19321341
NP1 Function assay Agonist activity at GR ligand binding domain expressed in human NP1 cells assessed as glucocorticoid response element transactivation by GAL4 luciferase reporter gene assay, EC50 = 0.0042 μM. 19321341
TH2 Function assay 48 hrs Inhibition of pro-inflammatory cytokine IL5 production in ovalbumin-stimulated BALB/c mouse TH2 cells after 48 hrs by sandwich-ELISA, IC50 = 0.005 μM. 19323483
TH2 Function assay 48 hrs Inhibition of pro-inflammatory cytokine IL13 production in ovalbumin-stimulated BALB/c mouse TH2 cells after 48 hrs by sandwich-ELISA, IC50 = 0.005 μM. 19323483
MDA-kb2 Function assay Agonist activity at androgen receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150 = 0.194 μM. 19592245
MDA-kb2 Function assay Agonist activity at glucocorticoid receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150 = 0.194 μM. 19592245
A549 Function assay Agonist activity at GR in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM. 19592247
COS7 Function assay Agonist activity at glucocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay, EC50 = 0.0072 μM. 19863083
A549 Function assay 6 hrs Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of IL-1-beta-induced NF-kappaB dependent E-selection promoter activation after 6 hrs by luciferase reporter gene based ELAM assay, EC50 = 0.0011 μM. 20047280
A549 Function assay 6 hrs Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of PMA-induced AP1 activity after 6 hrs by luciferase reporter gene assay, EC50 = 0.0025 μM. 20047280
HeLa Function assay Transactivation of GAL-4 tagged glucocorticoid receptor ligand binding domain expressed in human HeLa cells assessed as NP1 activation by luciferase reporter gene assay, EC50 = 0.0045 μM. 20047280
NIH-3T3 Function assay 0.01 mg/kg 1 hr Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.01 mg/kg, po after 1 hr, Cp = 0.044 μM. 20469868
NIH-3T3 Function assay 0.1 mg/kg 1 hr Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.1 mg/kg, po after 1 hr, Cp = 0.236 μM. 20469868
NIH-3T3 Function assay 1 mg/kg 1 hr Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 1 mg/kg, po after 1 hr, Cp = 1.8 μM. 20469868
NIH-3T3 Function assay 10 mg/kg 1 hr Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 10 mg/kg, po after 1 hr, Cp = 17.7 μM. 20469868
NIH-3T3 Function assay 0.01 mg/kg 1 hr Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.01 mg/kg, po after 1 hr, Fu = 0.00203 μM. 20469868
NIH-3T3 Function assay 0.1 mg/kg 1 hr Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.1 mg/kg, po after 1 hr, Fu = 0.0116 μM. 20469868
NIH-3T3 Function assay 1 mg/kg 1 hr Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 1 mg/kg, po after 1 hr, Fu = 0.087 μM. 20469868
NIH-3T3 Function assay 10 mg/kg 1 hr Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 10 mg/kg, po after 1 hr, Fu = 5.123 μM. 20469868
HeLa Function assay Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay, EC50 = 0.007943 μM. 20727743
HeLa Function assay Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay, IC50 = 0.001585 μM. 20727743
THP1 Function assay Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-8 production, IC50 = 0.002512 μM. 20727743
Sf9 Function assay Binding affinity to human recombinant glucocorticoid receptor expressed in baculovirus infected Sf9 cells, IC50 = 0.01259 μM. 20727743
insect cells Function assay Binding affinity to glucocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay, IC50 = 0.0034 μM. 20735001
insect cells Function assay Binding affinity to mineralocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay, IC50 = 0.033 μM. 20735001
U2OS Function assay 18 hrs Agonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as increase of transactivation activity after 18 hrs by luciferase reporter gene assay, EC50 = 15.8489 μM. 20812681
U2OS Function assay 18 hrs Antagonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay, IC50 = 0.0005082 μM. 20812681
HepG2 Function assay 24 hrs Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis, EC50 = 2.6 μM. 20966043
A549 Function assay Transrepression activity of glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM. 21073190
A549 Function assay Transrepression activity of glucocorticoid receptor in human A549 cells expressing AP-1 assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay, EC50 = 0.0025 μM. 21073190
NP-1 Hela Function assay Transactivation activity of glucocorticoid receptor ligand binding domain expressed in human NP-1 Hela cells co-expressing GAL4 DNA binding domain by luciferase reporter gene assay, EC50 = 0.0042 μM. 21073190
13D3/Huh7 Function assay 24 hrs Transactivation activity at glucocorticoid receptor in human 13D3/Huh7 cells assessed as induction of tyrosine aminotransferase activity after 24 hrs, EC50 = 0.005 μM. 21073190
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM. 21257309
A549 Function assay Agonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity, IC50 = 0.003981 μM. 21257309
RAW264.7 Antiinflammatory assay 18 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated 2 hrs before LPS challenge measured after 18 hrs by griess reaction, IC50 = 0.86 μM. 21288727
HMC1 Function assay 1 hr Immunomodulatory activity in human HMC1 cells assessed as inhibition of phorbol 12-myristate 13-acetate/A23187-stimulated IL1-beta secretion treated 1 hr prior to 30 mins phorbol 12-myristate 13-acetate/A23187 challenge by Western blotting analysis 21302967
RAW264.7 Antiinflammatory assay 10 uM 24 hrs Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as nitrite level at 10 uM after 24 hrs by Griess method, Activity = 1.54 μM. 21353543
RAW264.7 Antiinflammatory assay 18 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs, IC50 = 0.01 μM. 21353543
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess method, IC50 = 0.8 μM. 21353543
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction, IC50 = 0.02 μM. 21361338
RAW264.7 Function assay 20 mins Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells pre-incubated for 20 mins before LPS challenge measured 18 hrs post LPS challenge by Griess method 21775152
RAW264.7 Function assay 30 mins Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells pre-incubated for 30 mins before LPS challenge measured 6 hrs post LPS challenge by ELISA 21775152
HeLa Function assay Agonist activity at glucocorticoid receptor in human HeLa cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity, EC50 = 0.017 μM. 21963986
insect cells Function assay Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant glucocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.003 μM. 21963986
insect cells Function assay Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant mineralocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.033 μM. 21963986
RAW264.7 Antiinflammatory assay 2 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production pretreated for 2 hrs before LPS challenge measured after 18 hrs by Griess method, IC50 = 0.47 μM. 22372956
RAW264.7 Antiinflammatory assay 2 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production pretreated for 2 hrs before LPS challenge measured after 18 hrs by Griess method, IC50 = 0.98 μM. 22537362
A549 Antiinflammatory assay 1 uM 30 mins Antiinflammatory activity in human A549 cells assessed as inhibition of IL-1beta-induced mPGES1 expression at 1 uM treated 30 mins prior to IL-1beta challenge measured after 48 hrs by Western blot analysis relative to control 22795900
H13 Function assay 3 hrs Inhibition of glucocorticoid receptor in human H13 cells assessed as inhibition of glucocorticoid-induced cell proliferation after 3 hrs by [3H]-thymidine incorporation assay, EC50 = 0.0097 μM. 23199485
293 MSR Function assay 60 mins Displacement of [3H]-dexamethasone human glucocorticoid receptor alpha expressed in 293 MSR cells after 60 mins by scintillation counting, EC50 = 0.0125 μM. 23199485
IOBA-NHC Function assay 40 uM 24 hrs Inhibition of NF-kappaB p65-mediated IL-6 release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA 23219855
IOBA-NHC Function assay 40 uM 24 hrs Inhibition of NF-kappaB p65-mediated TNFalpha release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA 23219855
IOBA-NHC Function assay 40 uM 24 hrs Inhibition of NF-kappaB p65-mediated IL-8 release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA 23219855
HCLE Function assay 40 uM 24 hrs Inhibition of NF-kappaB p65-mediated IL-8 release in HSV1 KOS infected human HCLE cells at 40 uM after 24 hrs by ELISA 23219855
HCT116 Function assay 20 to 40 uM 24 hrs Agonist activity at glucocorticoid receptor (unknown origin) expressed in human HCT116 cells co-expressing GRE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay 23276449
RAW264.7 Antiinflammatory assay 2 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 2 hrs prior to LPS-challenge measured after 24 hrs by Griess method, IC50 = 1.43 μM. 23373965
HeLaS3 Function assay 2 hrs Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs, IC50 = 0.0041 μM. 23403082
HeLaS3 Function assay 2 hrs Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs, Ki = 0.0022 μM. 23403082
A549 Function assay Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM. 23916594
A549 Function assay Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-stimulated AP1 response element by luciferase reporter gene assay, EC50 = 0.0025 μM. 23916594
Hela Function assay Transactivation activity at glucocorticoid receptor ligand binding domain (unknown origin) expressed in human Hela cells co-expressing GAL4 DNA binding domain assessed as NP-1-stimulated GRE activation by luciferase reporter gene assay, EC50 = 0.0045 μM. 23916594
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL-1beta-induced NF-kappaB dependent E-selectin activation by luciferase reporter gene assay, EC50 = 0.0011 μM. 23953070
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activation by luciferase reporter gene assay, EC50 = 0.0025 μM. 23953070
HeLa Function assay Transactivation of glucocorticoid receptor ligand binding domain (unknown origin) transfected in human HeLa cells assessed as activation of NP-1 by GAL4 luciferase reporter gene assay, EC50 = 0.0045 μM. 23953070
A549 Function assay Transrepression of glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay, EC50 = 0.0025 μM. 24011644
HeLa Function assay Transactivation of GR-LBD expressed in human HeLa cells co-expressing GAL4-DBD by luciferase reporter gene assay, EC50 = 0.0042 μM. 24011644
HEK293 Function assay Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells, Ki = 0.00036 μM. 24446728
HEK293 Function assay Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells, Ki = 0.00069 μM. 24446728
HEK293 Function assay Displacement of [3H]-methyltrienolone from human progesterone receptor expressed in HEK293 cells, Ki = 0.561 μM. 24446728
HEK293 Function assay Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells, Ki = 1.41 μM. 24446728
HeLa Function assay Transactivation of glucocorticoid receptor in human HeLa cells harboring MMTV promoter by luciferase reporter gene assay, EC50 = 0.017 μM. 24656565
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells assessed as E-selectin transrepression by luciferase reporter gene assay, EC50 = 0.0011 μM. 24980053
A549 Function assay Agonist activity at glucocorticoid receptor in human A549 cells assessed as AP-1 transrepression by luciferase reporter gene assay, EC50 = 0.0025 μM. 24980053
HeLa Function assay Agonist activity at glucocorticoid receptor in human HeLa cells assessed as NP-1 transactivation by luciferase reporter gene assay, EC50 = 0.0045 μM. 24980053
B16F10 Antitumor assay 20 mg/kg 24 days Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as inhibition tumor growth at 20 mg/kg, ip measured after 24 days of tumor inoculation 24992071
B16F10 Antitumor assay 20 mg/kg 24 days Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as apoptotic regions at 20 mg/kg, ip measured after 24 days of tumor inoculation by TUNEL assay 24992071
B16F10 Apoptosis assay 10 uM 48 hrs Induction of apoptosis in mouse B16F10 cells assessed as increase in ratio of BAX/Bcl2 expression at 10 uM after 48 hrs by Western blot analysis relative to untreated control 24992071
B16F10 Antitumor assay 20 mg/kg 24 days Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as apoptotic regions at 20 mg/kg, ip measured after 24 days of tumor inoculation by VE-cadherin 24992071
CUTLL1 Growth inhibition assay 48 hrs Growth inhibition of human CUTLL1 cells with high GR expression levels after 48 hrs by alamar blue assay 25050160
HEK293 Function assay Agonist activity at human GCR expressed in HEK293 cells by luciferase reporter gene assay, EC50 = 0.0013 μM. 25305688
RAW264.7 Function assay 24 hrs Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay relative to vehicle-treated control, IC50 = 0.8 μM. 25499882
HFF Function assay Agonist activity at GR in HFF cells assessed as suppression of IL-1-induced IL-6 production, IC50 = 0.001 μM. 25516791
RAW264.7 Antiinflammatory assay 1 mM 30 mins Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction of LPS-induced TNF mRNA expression cells at 1 mM treated 30 mins before LPS challenge measured after 3 hrs by qRT-PCR analysis 25667960
SW1353 Function assay 24 hrs Transrepression activity at glucocorticoid receptor in human SW1353 cells assessed as repression of IL-1-induced MMP-13 production after 24 hrs by ELISA, IC50 = 0.0018 μM. 25706100
RAW264.7 Function assay 6 hrs Inhibition of TNFalpha production in mouse RAW264.7 cells incubated for 6 hrs by sandwich immunoassay, IC50 = 0.04 μM. 25824662
J774A.1 Function assay 6 hrs Inhibition of TNFalpha production in mouse J774A.1 cells incubated for 6 hrs by sandwich immunoassay, IC50 = 0.4 μM. 25824662
RAW264.7 Function assay 12 hrs Inhibition of IL-1beta production in mouse RAW264.7 cells incubated for 12 hrs by sandwich immunoassay, IC50 = 4.7 μM. 25824662
J774A.1 Function assay 12 hrs Inhibition of IL-1beta production in mouse J774A.1 cells incubated for 12 hrs by sandwich immunoassay, IC50 = 22 μM. 25824662
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 0.63 μM. 26087384
BV2 Antiinflammatory assay 24 hrs Antiinflammatory activity in C57BL6/J mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 0.025 μM. 26110443
RAW264.7 Function assay 24 hrs Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 0.8 μM. 26305406
J774 Antiinflammatory assay 10 uM 24 hrs Antiinflammatory activity against mouse J774 cells assessed as inhibition of LPS-induced iNOS expression at 10 uM after 24 hrs by Western blot analysis 26915998
IM9 Function assay Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM9 cells, IC50 = 0.0038 μM. 26988801
C57BL/6 Antiinflammatory assay 10 mg/kg 1 hr Antiinflammatory activity in C57BL/6 mouse assessed as inhibition of zymosan-induced mononuclear cells migration in articular cavity at 10 mg/kg, ip administered 1 hr prior to zymosan challenge measured at 6 to 24 hrs 27227459
C57BL/6 Antiinflammatory assay 10 mg/kg 1 hr Antiinflammatory activity in C57BL/6 mouse assessed as inhibition of zymosan-induced infiltration of inflammatory cells into synovial tissue at 10 mg/kg, ip administered 1 hr prior to zymosan challenge measured at 6 to 24 hrs by hematoxylin and eosin stai 27227459
J774A.1 Antiinflammatory assay 1 uM 1 hr Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced IL6 production in cell-free supernatant at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by sandwich ELISA 27227459
J774A.1 Antiinflammatory assay 1 uM 1 hr Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced COX2 expression at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by Western blot analysis 27227459
J774A.1 Antiinflammatory assay 1 uM 1 hr Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced nitric oxide production at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by colorimetric Griess test 27227459
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs in presence of LPS by Griess assay, IC50 = 0.63 μM. 27825545
IM9 Function assay Displacement of [3H]dexamethasone from GR receptor in human IM9 cells, IC50 = 0.0038 μM. 27876250
HeLa Function assay Transrepression activity at glucocorticoid receptorin human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay, IC50 = 0.001585 μM. 28043796
THP1 Function assay Transrepression activity at glucocorticoid receptor in human THP1 cells assessed as receptor-mediated anti-inflammatory activity by measuring inhibition of LPS-induced IL-8 production, IC50 = 0.002512 μM. 28043796
HeLa Function assay Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay, IC50 = 0.007943 μM. 28043796
Sf9 Function assay Binding affinity to recombinant human glucocorticoid receptor expressed in baculovirus infected sf9 cells, IC50 = 0.01259 μM. 28043796
RAW264.7 Antiinflammatory assay 30 mins Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced NO production pretreated for 30 mins followed by LPS stimulation for 24 hrs by Griess assay, IC50 = 7 μM. 28499733
RAW264.7 Function assay 24 hrs Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 2.5 μM. 28598633
Mino Antiproliferative assay 100 uM 48 hrs Antiproliferative activity against human Mino cells at 100 uM preincubated for 48 hrs followed by thymidine addition measure after 16 hrs by Thymidine incorporation assay 28858511
RAW264.7 Antiinflammatory assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by griess assay, IC50 = 0.8 μM. 29272126
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in COX2 mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in iNOS mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in TNFalpha mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR ana 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-1beta mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR ana 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-6 mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in NO production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by Grie 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-1beta production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs b 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-6 production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by EL 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in TNFalpha production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 3 hrs by 29389121
RAW264.7 Function assay 10 uM 1 hr Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in iNOS protein level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by 29389121
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BV2 Antiinflammatory assay Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production, IC50 = 9.5 μM. 29482940
RAW264.7 Function assay 24 hrs Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 10.7 μM. 29518326
HeLa Function assay 0.4 uM 24 hrs Transrepression of GCR in human HeLa cells assessed as suppression of DEX-induced GILZ mRNA expression at 0.4 uM after 24 hrs by Taqman-based real-time PCR analysis 29670697
RAW264.7 Antiinflammatory assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production, IC50 = 8.3 μM. 29741372
HEK 293T Function assay Agonist activity at GAL4 DNA-binding domain fused GR (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay, IC50 = 0.00235 μM. 30144697
RAW264.7 Antiinflammatory assay 20 uM 6 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA 30215255
RAW264.7 Antiinflammatory assay 20 uM 6 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-1beta production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA 30215255
RAW264.7 Antiinflammatory assay 20 uM 6 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA 30215255
RAW264.7 Antiinflammatory assay 20 uM 6 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA 30215255
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Biological Activity

Description Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients.
Targets
interleukin receptor [1]
(Cell-free assay)
In vitro
In vitro

Dexamethasone results in decrease in transmonolayer paracellular permeability mainly to sucrose, fluorescein and dextrans of up to 20 KDa in an immortalised rat brain endothelial cell line (GPNT). Dexamethasone results in filamentous actin and the cytoskeleton associated protein cortactin being highly concentrated in the regions of cell-cell contact with few F-actin stress fibres visible within the cytoplasm in cultured rat brain endothelial cells, an observation consistent with a more differentiated barrier phenotype induced by dexamethasone. Dexamethasone treatment has been shown to strongly stimulate the level of the Id-1 protein, which is a serum-inducible helix-loop-helix transcriptional repressor, involved in cell differentiation, and this effect was shown to be associated with reorganisation of ZO-1 to the cell periphery in Con8 mammary epithelial tumor cells. Dexamethasone prevents cytokine-induced enhanced expression of MMP-9 and alterations in the expression of ZO-1 in untreated GPNT monolayers. [1]

Dexamethasone depletes both basal and TNF-alpha-stimulated GSH levels by down-regulating the gamma-GCS-heavy subunit transcription via a mechanism involving AP-1 (c-Jun) in alveolar epithelial cells. Dexamethasone decreases both basal and stimulated GSH levels (TNF-α-treated) in alveolar epithelial cells (A549), without any change in GSSG. [2]
Cell Research Cell lines CB CD34+ cells
Concentrations 1 μM
Incubation Time 16 h
Method

Cells were treated with indicated concentrations of drug.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Bcl-2 / Bcl-xl / Mcl-1 / Survivin / IAP1 Cyclin D1 / Cyclin E / COX-2 / MMP-9 Bax / p21 p-JNK / JNK / p-p38 / p38 / p-ERK / ERK 28696369
In Vivo
In vivo

Dexamethasone is administered i.m. to pregnant ewes, leads to the following results (1) blood pressure is unchanged; (2) as previously reported in the fetus, sensitivity to endothelin-1 (ET) is increased; (3) acetylcholine-induced relaxation is increased; (4) L-NAME suppressible vasodilatory response to ET is abolished; (5) there is no change in endothelium-independent vasodilatation; and (6) there is no change in eNOS RNA and protein levels, when compared to saline treated controls. [3]
Animal Research Animal Models Mice
Dosages 1 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06118710 Not yet recruiting Cancer Erasmus Medical Center January 1 2024 Phase 4
NCT05759481 Not yet recruiting Post-operative Nausea and Vomiting Milton S. Hershey Medical Center January 2024 Phase 2
NCT06133712 Recruiting Carpal Tunnel|Dexmedetomidine|Ozone|Dexamethasone Tanta University November 1 2023 Not Applicable
NCT05994183 Withdrawn Bronchiolitis IDeA States Pediatric Clinical Trials Network|National Institutes of Health (NIH)|University of Nebraska October 9 2023 Early Phase 1

Chemical lnformation & Solubility

Molecular Weight 392.46 Formula

C22H29FO5
CAS No. 50-02-2 SDF Download Dexamethasone SDF
Smiles CC1CC2C3CCC4=CC(=O)C=CC4(C3(C(CC2(C1(C(=O)CO)O)C)O)F)C
Storage (From the date of receipt) Store at 4℃(in the dark)

In vitro
Batch:

DMSO : 78 mg/mL ( (198.74 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 11 mg/mL

Water : Insoluble


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In vivo
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Frequently Asked Questions

Question 1:
I'm loonkig for Dexamethasone to use in cell culture, would it be better to use the Dexamethasone S1322, the sodiume phosphate S4028 or the acetate S3124?

Answer:
S1322 is the free base form of Dexamethasone, S4028 is the sodium phosphate form and S3124 is the acetate salt. All of them have similar biological activity in tissue culture, however, their suitabilities vary in different solvents. As free base, S1322 has high solubility in DMSO (79mg/ml), poor solubility in water (<1mg/ml), and moderate solubility in ethanol (6mg/ml). As sodium phosphate salt, S4028 has high solubility in water (103mg/ml) but is insoluble in DMSO and ethanol (<1mg/ml). The solubility of S3124 is 87mg/ml in DMSO, <1mg/ml in water, and 20mg/ml in ethanol. Selection can be made based on the customer's experimental setup.

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