k373

GSK3739936 is a potent inhibitor of HIV-1 allosteric integrase (IC50: 11.1 nM, EC50: 1.7 nM). GSK3739936 is also a weak inhibitor of CYP with an IC50 >24.3 μM. It has good pharmacokinetic properties with rapid absorption, low to moderate clearance and good oral bioavailability.

GSK3735967 is a selective, reversible, non-nucleoside inhibitor targeting DNMT1, demonstrating an IC50 value of 40 nM. It features a planar dicyanopyridine core designed to specifically interact with DNMT1-bound hemimethylated CpG dinucleotides. Additionally, GSK3735967 possesses three binding sites, with one uniquely capable of binding to histone H4K20me3 [1] [2].

UNC0224 is a selective inhibitor of G9a with a Ki of 2.6 nM and IC50 of 15 nM. UNC0224 also potently inhibits GLP with assay-dependent IC50 values of 20-58 nM.

UNC0321 is an effective inhibitor of histone methyltransferase G9a with a Ki of 63 pM and with IC50s 9 nM and 6 nM in ECSD and CLOT assays. UNC0321 inhibits GLP with IC50s of 15 nM and 23 nM in ECSD and CLOT assays.

SIRT7 inhibitor 97491 is an HDAC inhibitor with high specificity for SIRT7 (IC50 = 325 nM). SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway.