Home Cytoskeletal Signaling Sirtuin inhibitor AGK2 For research use only.

AGK2

AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.

AGK2 Chemical Structure

AGK2 Chemical Structure

CAS: 304896-28-4

Selleck's AGK2 has been cited by 30 Publications

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Purity & Quality Control

Batch: Purity: 99.98%
99.98

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa Function assay Inhibition of over-expressed SIRT2 immunoprecipitated from HeLa cells transfected with SIRT2-myc expression construct 17588900
H4 Function assay 24 hrs Inhibition of SIRT2 in H4 cells co-transfected with alphaSyn and synphilin1 assessed as enlarged alphaSyn inclusions after 24 hrs 17588900
rat embryo midbrain Function assay Protection of dopaminergic cell death in rat embryo midbrain transduced with lentivirus encoding alphaSyn-A53T mutant assessed as tyrosine hydroxylase positive cells 17588900
HCT116 Function assay 10 uM 8 hrs Inhibition of SIRT2 in human HCT116 cells assessed as increase in acetylated alpha-tubulin at 10 uM after 8 hrs by Western blot analysis 22642300
Escherichia coli cells Function assay Inhibition of human recombinant SIRT2 expressed in Escherichia coli cells using acetylated Lys side chain amino acids 379-382 (Arg-His-Lys-Lys(Ac)) p53 conjugated with aminomethylcoumarin as substrate by fluorescence assay, IC50=5.5μM 22931526
30PT Cytotoxicity assay 72 hrs Cytotoxicity against human 30PT cells after 72 hrs by Cell-titer GLo assay, CC50=9.6μM 22931526
30P Cytotoxicity assay 72 hrs Cytotoxicity against human 30P cells after 72 hrs by Cell-titer GLo assay, CC50=12.5μM 22931526
Escherichia coli cells Function assay Inhibition of human recombinant SIRT1 expressed in Escherichia coli cells using acetylated Lys side chain amino acids 379-382 (Arg-His-Lys-Lys(Ac)) p53 conjugated with aminomethylcoumarin as substrate by fluorescence assay, IC50=38μM 22931526
30PT Cytotoxicity assay 72 hrs Cytotoxicity against human 30PT cells after 72 hrs by celltiter-glo luminescent assay, CC50=9.6μM 23189967
30P Cytotoxicity assay 72 hrs Cytotoxicity against human 30P cells after 72 hrs by celltiter-glo luminescent assay, CC50=12.5μM 23189967
Escherichia coli BL21 (DE3) Function assay Inhibition of full length human SIRT2 expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay, IC50=1.56μM 25275824
SH-SY5Y Neuroprotective assay 1 to 10 uM 30 mins Neuroprotective activity against oligomeric alpha-synuclein-induced cytotoxicity in human SH-SY5Y cells assessed as increase in cell growth at 1 to 10 uM preincubated for 30 mins followed by alpha-synuclein addition measured after 72 hrs by MTT assay 26982234
MCF7 Function assay 10 to 50 uM 24 hrs Inhibition of SIRT2 in human MCF7 cells assessed as increase in alpha-tubulin K40 acetylation level at 10 to 50 uM after 24 hrs in presence of TSA by Western blot analysis 28135086
U373 Antiproliferative assay 72 hrs Antiproliferative activity against human U373 cells after 72 hrs by MTT assay, IC50=47.6μM 28475330
Hs683 Cell cycle assay 24 to 48 hrs Cell cycle arrest in human Hs683 cells assessed as accumulation at sub-G1 phase at IC50 for MTT assay after 24 to 48 hrs by propidium iodide staining-based flow cytometry 28475330
U373 Cell cycle assay 24 to 48 hrs Cell cycle arrest in human U373 cells assessed as accumulation at sub-G1 phase at IC50 for MTT assay after 24 to 48 hrs by propidium iodide staining-based flow cytometry 28475330
Hs683 Cell cycle assay 24 to 48 hrs Cell cycle arrest in human Hs683 cells assessed as accumulation at G2/M phase at IC50 after 24 to 48 hrs by propidium iodide staining-based flow cytometry 28475330
U373 Cell cycle assay 24 to 48 hrs Cell cycle arrest in human U373 cells assessed as accumulation at G2/M phase at IC50 after 24 to 48 hrs by propidium iodide staining-based flow cytometry 28475330
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Biological Activity

Description AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM that minimally affects either SIRT1 or SIRT3 at 10-fold higher levels.
Targets
SIRT2 [1]
(Cell-free assay)
3.5 μM
In vitro
In vitro In SIRT2-myc-expressing HeLa cells, AGK2 effectively inhibits the activity of SIRT2, and increases acetylated tubulin. AGK2 protects dopaminergic neurons from α-Syn–induced toxicity in primary midbrain cultures. [1] AGK2 induces both necrosis and caspase-3-dependent apoptosis in C6 glioma cells. [2] SIRT2 also decreases merlin-mutant viability of mouse schwann cells (MSCs) without substantially reducing wild-type MSC viability. [3]
In Vivo
In vivo In drosophila model of parkinson's disease, AGK2 rescues α-Syn–mediated toxicity and modify aggregation. [1]
Animal Research Animal Models Drosophila model of parkinson
Dosages 1mM
Administration --

Chemical lnformation & Solubility

Molecular Weight 434.27 Formula

C23H13Cl2N3O2
CAS No. 304896-28-4 SDF Download AGK2 SDF
Smiles C1=CC2=C(C=CC=N2)C(=C1)NC(=O)C(=CC3=CC=C(O3)C4=C(C=CC(=C4)Cl)Cl)C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 4 mg/mL ( (9.21 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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