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.