| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H13Cl2N3O2 |
| Molecular Weight | 434.274 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
ClC1=CC=C(Cl)C(=C1)C2=CC=C(O2)\C=C(/C#N)C(=O)NC3=CC=CC4=NC=CC=C34
InChI
InChIKey=SVENPFFEMUOOGK-SDNWHVSQSA-N
InChI=1S/C23H13Cl2N3O2/c24-15-6-8-19(25)18(12-15)22-9-7-16(30-22)11-14(13-26)23(29)28-21-5-1-4-20-17(21)3-2-10-27-20/h1-12H,(H,28,29)/b14-11+
| Molecular Formula | C23H13Cl2N3O2 |
| Molecular Weight | 434.274 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Optical Activity | NONE |
The histone deacetylases (HDACs), Sirtuin 1 (Sirt1) and Sirt2, play crucial roles in many biological processes, including cell proliferation, differentiation, and apoptosis. AGK2 is a cell-permeable, selective inhibitor of sirtuin 2 (SIRT2), which as was shown, prevented cellular α-tubulin deacetylation in HeLa cells in a dose-dependent manner and with little cytotoxic effect. AGK2 can be a useful tool for studying the roles of SIRT2 in neurodegeneration and aging, as well as cell cycle progression and tumorigenesis.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 3.5 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
PubMed
Sample Use Guides
It was examined insoluble, polymerized microtubules and soluble alpha-tubulin after treatment of HeLa cells with either AGK2 or AGK3, a less potent structural analog of AGK2, for 3 hours. A dose dependent increase in acetylated tubulin was observed in both fractions of AGK2 treated cells relative to untreated or AGK3-treated cells. Thus, AGK2 could enter cells and act on endogenous SIRT2 in its native environment. AGK2 (5, 10, 20, 30, 40, 50 Um) treatment results in a dose-dependent increase in acetylation of soluble tubulin monomers (S) and polymerized microtubules (P) in fractionated HeLa cell extracts. The effect of the less potent SIRT2 inhibitor AGK3 was shown for comparison.
