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UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC50 of 38 μM. UBCS039 induces deacetylation of SIRT6-targeted histone H3 sites in human cancer cells. UBCS039-mediated activation of autophagy was strictly dependent on SIRT6 deacetylating activity since the catalytic mutant H133Y failed to activate autophagy.
| Cell Experiment | |
|---|---|
| Cell lines | HeLa cells |
| Preparation method | HeLa cells were treated with 100 µM UBCS039 for 24 h, detached, and disrupted by three cycles of freezing-thawing in dry ice with ethanol in a buffer containing 100 mM Tris-HCl, pH 7.75, and 4 mM EDTA. |
| Concentrations | 100 µM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6 mice |
| Formulation | Not mentioned |
| Dosages | 50 mg/kg |
| Administration | Intraperitoneal injection |
| Molecular Weight | 247.29 |
| Formula | C16H13N3 |
| CAS Number | 358721-70-7 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Sirtuin Products |
|---|
| Selisistat
Selisistat (EX 527) is a potent and selective SIRT1 class III histone deacetylase enzyme inhibitor with an IC50 of 98 nM. |
| SRT1720 Hydrochloride
SRT1720 Hydrochloride is a selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol (EC1.5 = 0.16 versus 46.2 µM, respectively). SRT1720 increased the activity of SIRT1 and AMPKα phosphorylation at Ser485 via the cAMP-protein kinase A (PKA) pathway. |
| Resveratrol
Resveratrol is a phytoestrogen with antitumor, antioxidant, antiplatelet, anti-inflammatory and antifungal effects. |
| Balsalazide disodium
Balsalazide is an anti-inflammatory compound used to study inflammatory bowel disease and ulcerative colitis. |
| Sirtinol
Sirtinol is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM, respectively. |
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