JYQ-42 | SIRT6 inhibitor | Probechem Biochemicals

Chemical Structure : JYQ-42

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JYQ-42 (SIRT6 inhibitor JYQ42)

货号: PC-49248Not For Human Use, Lab Use Only.

JYQ-42 is a potent, selective SIRT6 allosteric inhibitor, effectively inhibits SIRT6 deacetylation with IC50 of 2.33 uM, inhibits the deacetylation activity of SIRT6 in pancreatic cancer cell lines.

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生物&药学活性

JYQ-42 is a potent, selective SIRT6 allosteric inhibitor, effectively inhibits SIRT6 deacetylation with IC50 of 2.33 uM, inhibits the deacetylation activity of SIRT6 in pancreatic cancer cell lines.
JYQ-42 is a non-competitive inhibitor with high selectivity for targeting SIRT6, shows high selectivity over 17 HDACs, including other sirtuins.
JYQ-42 effectively inhibits the SIRT6 deacetylation activity on H3K9Ac with IC50 of 9.1 uM.
JYQ-42 inhibits SIRT6 through the newly identified allosteric exosite Pocket Z with Kd of 22.07 uM in SPR assays.
JYQ-42 inhibits SIRT6 deacetylation and cell migration of pancreatic cancer cells, increases the levels of H3K9Ac, H3K18Ac and H3K56Ac in a dose-dependent manner in BXPC-3 and MiaPaCa-2 cell lines.
JYQ-42 (5 uM) dramatically attenuates cell migration of and cytokine production in pancreatic cancer cells, with no significant impact on cell growth.
JYQ-42 inhibits the expression and secretion of inflammatory factors, significantly reduces the expression of IL6, IL8 and TNF-α in BXPC-3 cells in a dose-dependent manner.

物理化学性质&存储条件

分子量	400.706
分子式	C13H8ClF3N8O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(E)-1-(4-amino-1,2,5-oxadiazol-3-yl)-N'-(3-chloro-5-(trifluoromethyl)benzylidene)-1H-1,2,3-triazole-4-carbohydrazide

参考文献

1. Qiufen Zhang, et al. Acta Pharm Sin B. 2022 Feb;12(2):876-889.

JYQ-42 (SIRT6 inhibitor JYQ42)

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JYQ-42 (SIRT6 inhibitor JYQ42)

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