Home GPCR & G Protein cAMP activator - FXR activator - Autophagy activator Forskolin (Colforsin) For research use only.

Forskolin (Colforsin)

Synonyms: HL 362, Coleonol

Forskolin (Colforsin) is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types, commonly used to raise levels of cAMP in the study and research of cell physiology. Forskolin also activates PXR and FXR activity. Forskolin stimulates autophagy.

Forskolin (Colforsin) Chemical Structure

Forskolin (Colforsin) Chemical Structure

CAS: 66575-29-9

Selleck's Forskolin (Colforsin) has been cited by 147 publications

Purity & Quality Control

Batch: Purity: 99.20%
99.20

Products often used together with Forskolin (Colforsin)

SQ22536

SQ22536 inhibits the elevation of cAMP content and adenylyl cyclase activity caused by forskolin.

Gao Y, et al. Eur J Pharmacol. 2001 Apr 20;418(1-2):111-6.

VPA (Valproic acid)

VPA significantly decreases PKA-dependent enhancement of mossy fiber transmission, following activation of adenylyl cyclase with forskolin.

Chang P, et al. Epilepsia. 2010 Aug;51(8):1533-42.

RepSox (E-616452)

RepSox and Forskolin along with other chemical cocktails are used together in reprogramming and chemical induction of iPSCs

Xie X, et al. Curr Opin Genet Dev. 2017 Oct;46:104-113.

TTNPB

TTNPB and Forskolin along with other small molecules can convert human urine cells into neurons directly, without introducing the transcription factors or miRNAs.

Xu G, et al. Sci Rep. 2019 Nov 13;9(1):16707.

EPZ004777

EPZ004777 and Forskolin are used in combination with other small molecules as cocktail in the medium for direct reprogramming of mouse fibroblasts into ciNCCs and ciCECs

Pan SH, et al. Sci Adv. 2021 Jun 4;7(23):eabg5749.

Related compound libraries

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT-29  Apoptosis Assay 40 μM 48 h DMSO induces changes in the phosphorylation status of PP2A targets 24997451
SW480 Apoptosis Assay 40 μM 48 h DMSO induces changes in the phosphorylation status of PP2A targets 24997451
HT-29  Apoptosis Assay 40 μM 48 h DMSO induces an activation of caspase 3/7 24997451
SW480 Apoptosis Assay 40 μM 48 h DMSO induces an activation of caspase 3/7 24997451
HT-29  Function Assay 40 μM 7 d DMSO reduces colonosphere formation capability  24997451
SW480 Function Assay 40 μM 7 d DMSO reduces colonosphere formation capability  24997451
HT-29  Growth Inhibition Assay 40 μM 0-72 h DMSO inhibits cell growth time dependently 24997451
SW480 Growth Inhibition Assay 40 μM 0-72 h DMSO inhibits cell growth time dependently 24997451
HT-29  Function Assay 40 μM 48 h DMSO activates PP2A 24997451
SW480 Function Assay 40 μM 48 h DMSO activates PP2A 24997451
C6 Function Assay 10 μM  20 min increases cAMP accumulation 25069417
Huh-7 Function Assay 0-20 μM 2 h  results in a dose-dependent increase in c-Myc expression at the protein and mRNA levels 25109834
THP-1  Function Assay 1/10 μM 2 h DMSO  suppresses MCP-1 production  25154882
BeWo  Function Assay 20 µM 48 h DMSO  induces cell fusion 25184477
ventricular cardiomyocytes  Function Assay 0.01-10 μM evokes an inotropic response 120±15% above basal with an EC50 of 2.2 µM 25203113
ventricular cardiomyocytes  Function Assay 0.01-10 μM increases cAMP accumulation 25203113
MIN6  Function Assay 10 μM  3 h increases D3 mRNA expression 25241124
L6 Function Assay 40 µM 24 h inhibits DMH1-induced Akt activation 25247550
HEK‐CFTR Function Assay 2–50 μM 0-12 min DMSO  induces a dose‐dependent iodide efflux  25263207
SK-N-SH Cell Viability Assay 10 μM  48 h enhances SK-N-SH neuroblastoma cell viability 25266063
SK-N-AS  Function Assay 10 μM  10/30/60 min increases levels of p-β-catenin (ser675) and induces accumulation of p-β-catenin (ser675) in (peri)nuclear regions 25266063
SK-N-AS  Function Assay 10 μM  30 min induces phosphorylation of β-catenin (ser675), p-GSK3β (ser9) and concomitant higher levels of active, unphosphorylated, β-catenin 25266063
SK-N-AS  Function Assay 10 μM  24 h increases the expression of cyclin D1 25266063
SK-N-AS  Function Assay 10 μM  24 h increases the cAMP levels  25266063
SK-N-AS  Cell Viability Assay 10 μM  24/48 h enhances time-dependently cellular viability  25266063
granulosa cells Function Assay 10 μM 24 h increases the levels of RGS2 promoter activity 25339105
granulosa cells Function Assay 10 μM 24 h increases the intensity of DNA/protein complex 25339105
granulosa cells Function Assay 10 μM 12/24 h increases the levels of reporter activity for the longest fragment (−854/+18RGS2.LUC) 25339105
granulosa cells Function Assay 10 μM 12/24 h increases the levels of RGS2 mRNA 25339105
BeWo  Function Assay 20 µM 48 h  DMSO  downregulates the level of GCM-1 25362260
BeWo  Function Assay 20 µM 48 h  DMSO  downregulates the level of TMEMF16 25362260
BeWo  Function Assay 20 µM 48 h  DMSO  increases the beta-hCG release 25362260
EM1  Function Assay 15 μM 48 h reduces the expression of LIF or PTGS2 in CALR- or EPAC2-silenced EM1 cells  25378661
Primary bovine chondrocytes Growth Inhibition Assay 5μM 48 h reverses the inhibitory effect of celecoxib on proliferation in growth plate chondrocytes 25406016
RBMECs Function Assay 5 μM 1 h blocks the actin cytoskeleton rearrangement seen with EMAP-II treatment  25416651
RBMECs Function Assay 5 μM 1 h blocks the EMAP-II-induced change in MLC phosphorylation 25416651
RBMECs Function Assay 5 μM 1 h reverses the changes in ZO-1 distribution seen with EMAP-II treatment 25416651
RBMECs Function Assay 5 μM 1 h inhibits the decreased of amount of ZO-1 in MFs induced by EMAP-II 25416651
RBMECs Function Assay 5 μM 1 h prevents the increase in HRP flux across the BTB induced by EMAP-II 25416651
RBMECs Function Assay 5 μM 1 h prevents the EMAP-II-induced TEER value decrease 25416651
RBMECs Function Assay 5 μM 1 h blocks the activation of RhoA/ROCK induced by EMAP-II 25416651
RBMECs Function Assay 0.05/0.5/5 μM 0.25 h increases cAMP concentration 25416651
ThGCs  Function Assay 10 μM 3 h inhibits the effect of H2O2 on EDN2 mRNA 25433027
ThGCs  Function Assay 10 μM 4 h increases CoCl2-induced EDN2 gene expression 25433027
ThGCs  Function Assay 10 μM 4 h augments HIF1A levels that were stimulated by CoCl2 25433027
LNCaP  Function Assay 10 μM 12 h  DMSO induces a dramatic increase of CREB1 activity 25548099
BeWo Function Assay 20 µM 48 h DMSO increases the adhesion of THP-1 monocytes 25566740
BeWo Function Assay 20 µM 48 h DMSO increases the differentiation of BeWo cells 25566740
OCI-Ly18  Function Assay 40 μM 1 h  DMSO induces the increment of cAMP concentrations 25576220
OCI-Ly1  Function Assay 40 μM 1 h  DMSO induces the increment of cAMP concentrations 25576220
3T3-L1 Function Assay 2.5/5 μM 24 h  significantly decreases ATGL protein expression at all doses tested 25590597
HEK293  Function Assay 5 µM 30 min increases cAMP levels 25591908
hADSCs Function Assay 5 µM 30 min increases cAMP levels 25591908
SH-SY5Y  Function Assay 10 μM 1 h  increases AGC1 mRNA level 25597433
SH-SY5Y  Function Assay 10 μM 1 h  increases LUC activity 25597433
UACC-647  Function Assay 10 μM 15 min DMSO increases eEF2 phosphorylation levels  25703025
UACC-647  Function Assay 10 μM 15 min DMSO inhibits ERK phosphorylation 25703025
UACC-647  Function Assay DMSO leads to a rise in cAMP levels (EC50 = 20.39 μM) 25703025
SC Function Assay 0.5 μM 72 h increases both Krox-20 and O1 expression in axon-related SCs but only Krox-20  25705874
SC Function Assay 0.5 μM 24 h mimicks the effect of cAMP analogs on O1 and MBP expression 25705874
oocytes Function Assay 5 μM 24 h attenuates rh-insulin action on oocyte GVBD significantly  25707854
BeWo Function Assay 10 μM  72 h DMSO mediates BeWo cell differentiation 25713425
GH3 Function Assay 1 μM 6-h induces PRL and Bmal1, but not Clock, mRNA expression 25727018
GH3 Function Assay 1 μM 6-h attenuates the correlation between PRL and Bmal1 expression 25727018
PC12 Function Assay 25 μM 48 h activates cAMP 25769305
BAECs Function Assay 25 μM 24 h enhances the activation of PPARα by 5 μM resveratrol, T4HS, or 4-PAP 25798826
GLUTag  Function Assay 10 µM 4 h increases the pCREB levels with the IBMX 25832631
GLUTag  Function Assay 10 µM 0/2/4 h stimulates GLP-1 secretion cotreated with IBMX 25832631
PBMC Function Assay 50 μM 24 h  inhibits the increased secretion of TNF induced by the DPE 25866079
H295R  Function Assay 10 μM 48 h increases steroid metabolites in the androgen, mineralo- and glucocorticoid pathways 25869556
3T3-L1 preadipocytes Function Assay 10 μM  12 h induces CREB phosphorylation and C/EBPβ expression 25928058
PCCL3 Function Assay 10 µM 24 h enhances DuOx2 promoter transcription activity ​ 25960956
SCG Function Assay 100 μM  DMSO reduces the excitability of SCG neurons 25962132
HEK-293 Function Assay 35 μM  DMSO induces a conspicuous “inactivation” of the Kv2.1 current 25962132
SCG Function Assay 20 μM  DMSO reversibly suppresses IKV with a IC50 of 24.4 μM 25962132
PC-3 Cell Viability Assay 40 µM 24/48/72 h DMSO decreases cell viability time dependently 26023836
PC-3 Function Assay 40 µM 2 h DMSO leads to PP2A activation 26023836
SH-SY5Y Function Assay 30 μM 30 min DMSO significantly increases the activation of PKA 26025137
EndoC-βH1 Function Assay 5 μM 1 h leads to a strong cAMP increase 26028562
EndoC-βH1 Function Assay 5 μM 1 h potentiates glucose-induced insulin secretion in the presence of glucose 26028562
RBMECs Function Assay 5 μM 1 h inhibits EMAP-II-induced inactivation of Rap1  26044663
AML-12  Function Assay 20 μM 3 h induces the dephosphorylation of CRTC2  26048985
AML-12  Function Assay 20 μM 3 h up-regulates Pgc1a, Pepck, and G6pc mRNA levels 26048985
AML-12  Function Assay 20 μM 1-8 h increases glucose production 26048985
AML-12  Function Assay 20 μM 3 h upregulates the phosphorylation levels at Thr-411 and Ser-493 26048985
Caco-2  Function Assay 0.1/1/10 μM 24 h increases MRP2 protein level 26049102
Caco-2  Function Assay 0.1/1/10 μM 20 min induces a dose-dependent increase in intracellular cAMP levels 26049102
bovine oocytes Function Assay 100 μM 12 h inhibits the effect of NPPA and/or NPPC to stimulate resumption of meiosis 26051611
BeWo  Function Assay 25 μM 24/48/72 h leads to an increase in the expression of other fusion markers 26053549
Spinal cords  Function Assay 1 μM 30 min stimulates cAMP levels 26126926
MDCK  Function Assay 10 µM 24 h DMSO inhibits the increased expression of FN caused by TGF-β1 26202352
MDCK  Function Assay 10 µM 24 h DMSO upregulates the expression of TGF-β1 and CTGF  26202352
RPMI 8226 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
H929 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
U266 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
OPM-2 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
INA-6 Cell Viability Assay 0-100 μM 72 h induces cell death dose dependently 26306624
RBMECs  Function Assay 5 μM 1 h blocks the Rac1 inactivation induced by EMAP-II 26358039
Mo-DCs Function Assay 50 μM 24 h promotes IL-23 production in the supernatant of zymosan stimulated Mo-DCs  26412948
HEK293 Function Assay 10 μM 6 h increases phosphorylation of overexpressed KLHL3 at S433 26435498
ASK Function assay 1 hr 2849641
Vero E6 Antiviral assay 17663539
epithelial cells Function assay 1 uM 4, 6, and 8 days 19966789
HepG2 (DPX-2) Function assay 24 hrs 20966043
HepG2 Function assay 24 hrs 20966043
HepG2 (DPX-2) Function assay 24 hrs 20966043
HEK293T Function assay 10 uM 24387325
HEK293 Function assay 10 uM 16 hrs 26435512
MCF7 Cytotoxicity assay 48 hrs 28838692
HEK293 Function assay 30 mins 30006176
Click to View More Cell Line Experimental Data

Biological Activity

Description Forskolin (Colforsin) is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types, commonly used to raise levels of cAMP in the study and research of cell physiology. Forskolin also activates PXR and FXR activity. Forskolin stimulates autophagy.
Targets
Adenylyl cyclase (AC) [1]
(A wide variety of cell types)
In vitro
In vitro

Forskolin increases cAMP levels in preparations of membranes, cells, or tissues. Forskolin not only activates AC but also interacts with certain other proteins, including glucose transporters and ion channels. Forskolin is able to promote activation of nine different transmembrane iso-forms of AC, albeit with somewhat less efficacy for AC9, which could be used to provides a means to identify and quantify high-affinity binding sites, i.e., G-proteins (Gs)–AC complexes. Activation of s by GPCRs contributes to Forskolin-stimulated cAMP generation in cells because of s-Forskolin potentiation of AC activity. [1] Forskolin stimulates adenylate cyclase activity without interacting with cell surface receptors. Forskolin's potentiation of cAMP in turn inhibits basophil and mast cell degranulation and histamine release, lowers blood pressure and intraocular pressure, inhibits platelet aggregation, promotes vasodilation, bronchodilation, and thyroid hormone secretion, and stimulates lipolysis in fat cells. Forskolin inhibits the binding of platelet-activating factor (PAF), independently of cAMP formation, which may be a result of Forskolin's direct effect on PAF or via interference with PAF binding to receptor sites. Forskolin also appears to have an effect on several membrane transport proteins, and inhibits glucose transport in erythrocytes, adipocytes, platelets, and other cells. Forskolin is used to treat with glaucoma. [2]
Cell Research Cell lines hMPCs or cynMPCs
Concentrations 20 μM
Incubation Time 2 h
Method

Cells were treated with 20 μM forskolin (S2449, Selleck) for 2 h for synchronization.
Experimental Result Images Methods Biomarkers Images PMID
Western blot cleaved caspase-3 / caspase-3 cleaved caspase-9 / caspase-9 β-catenin c-myc / Cyclin D1 pS6K1 / S6K1 / pCREB / CREB p-JNK / JNK / P-p38 / p38 30863177
Immunofluorescence 5hmC Fe(II) CYP17A1 / CYP21A2 29239726
Growth inhibition assay Cell viability 30863177
In Vivo
In vivo

Colforsin (Forskolin, HL 362, Coleonol) is a ubiquitous activator of eukaryotic adenylyl cyclase (AC) in a wide variety of cell types, commonly used to raise levels of cAMP. It also activates PXR and FXR activity and stimulates autophagy.[4]
Animal Research Animal Models Male Sprague-Dawley rats
Dosages 10 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04254705 Withdrawn Cystic Fibrosis Universitaire Ziekenhuizen KU Leuven|Vertex Pharmaceuticals Incorporated|KU Leuven|University of Lisbon March 1 2020 Not Applicable
NCT02807415 Completed Cystic Fibrosis Hannover Medical School|Heidelberg University|University of Giessen June 1 2016 --
NCT02586883 Completed Idiopathic Dilation of the Bronchi Assistance Publique - Hôpitaux de Paris March 29 2016 Not Applicable
NCT03652090 Completed Cystic Fibrosis Institut National de la Santé Et de la Recherche Médicale France|ABCF2 September 1 2010 --

Chemical lnformation & Solubility

Molecular Weight 410.5 Formula

C22H34O7
CAS No. 66575-29-9 SDF Download Forskolin (Colforsin) SDF
Smiles CC(=O)OC1C(C2C(CCC(C2(C3(C1(OC(CC3=O)(C)C=C)C)O)C)O)(C)C)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 82 mg/mL ( (199.75 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 82 mg/mL

Water : Insoluble


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In vivo
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