Cas No.: | 358721-70-7 |
Chemical Name: | 4-(pyridin-3-yl)-4,5-dihydropyrrolo[1,2-a]quinoxaline |
Synonyms: | UBCS-039;UBCS 039 |
SMILES: | N12C=CC=C1C(C1=CC=CN=C1)NC1=C2C=CC=C1 |
Formula: | C16H13N3 |
M.Wt: | 247.301 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | [1]. Weijie You, et al. Structural Basis of Sirtuin 6 Activation by Synthetic Small Molecules. Angew. Chem. Int. Ed. 2017, 56, 1007-1011. [2]. Sara Iachettini, et al. Pharmacological activation of SIRT6 triggers lethal autophagy in human cancer cells. Cell Death and Disease (2018) 9:996. |
Description: | UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC50 of 38 μM[1]. |
Target: | SIRT6:38 μM (EC50) |
In Vitro: | UBCS039 (75 μM, 48 or 72 hours) induces deacetylation of SIRT6-targeted histone H3 sites in human cancer cells[2]. UBCS039 leads to autophagosome accumulation in human cancer cells[2]. UBCS039 induces autophagy via AMP-activated protein kinase (AMPK) signaling pathway activation[2]. Western Blot Analysis[2] Cell Line: Human H1299 cells. Concentration: 75 μM. Incubation Time: 48 and 72 hours. Result: Induced deacetylation of SIRT6-targeted histone H3 sites in human H1299 cells. Western Blot Analysis[2] Cell Line: Human H1299 cells. Concentration: 75 μM. Incubation Time: 48 and 72 hours. Result: Induced deacetylation of SIRT6-targeted histone H3 sites in human H1299 cells. Cell Proliferation Assay[2] Cell Line: Human H1299 cells. Concentration: 100 μM. Incubation Time: 48 and 72 hours. Result: Led to a strong decrease of cell proliferation in a dose-dependent manner when compared with control or DMSO-treated cells, starting from day 3 of growth (48 h after treatment) in both H1299 and HeLa cell lines. |
References: | [1]. Led to a strong decrease of cell proliferation in a dose-dependent manner when compared with control or DMSO-treated cells, starting from day 3 of growth (48 h after treatment) in both H1299 and HeLa cell lines. [2]. Sara Iachettini, et al. Pharmacological activation of SIRT6 triggers lethal autophagy in human cancer cells. Cell Death and Disease (2018) 9:996. |