|Description||EPZ005687 is a selective EZH2 enzyme inhibitor with Ki of 24 nM. It is 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases. EPZ005687 can block trimethylation of the PRC2 target histone 3 lysine 27 with IC50 value of 80 nM, decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2. No development of preclinical research for the treatment of Cancer, Lymphoma and Solid tumours was reported.|
|Appearance||White to off-white Solid|
|Solubility||DMSO: ≤ 9.4 mg/mL|
|Application||Cancer; Lymphoma; Solid tumours|
|Quality Standard||In-house standard|
|Shelf Life||2 month in rt, long time|
|Current Developer||Eisai Co Ltd; Epizyme|
3-Deazaneplanocin A (DZNep), an inhibitor of S-adenosylmethionine-dependent methyltransferase that targets the degradation of EZH2.
UNC1999, the first orally bioavailable inhibitor that has high in vitro potency for wildtype and mutant EZH2 as well as EZH1. UNC1999 was highly selective for E...
CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
EI1 inhibits cellular H3K27 methylation and activates Ezh2 target gene p16 expression.
CPI-169 is a novel and potent EZH2 inhibitor, it decreases cellular levels of H3K27me3 and triggers cell cycle arrest and apoptosis in a variety of cell lines.
ZLD1039 potent, highly selective, and orally bioavailable small molecule inhibitor of EZH2, which inhibited the methyltransferase activity of EZH2 with high se...
GSK-503 is a potent EZH2 inhibitor with potential anticancer activity. Increased activity of the epigenetic modifier EZH2 has been associated with different can...
3-deazaneplanocin A (DZNeP) HCl
3-deazaneplanocin A (DZNeP)HCl, an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.
EPZ011989 trifluoroacetate is the trifluoroacetate salt form of EPZ011989. EPZ011989 is a potent and orally bioavailable inhibitor that specifically targets the...
EPZ-6438 is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. EPZ-6438 induces apoptosis and differentiation ...
GSK343 is a potent, selective inhibitor of EZH2 with cellular activity. GSK343 inhibits EZH2 with an IC50 of 4nM and is over 1000-fold selective for other HMTs...
GSK126 is a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity. GSK126 decreases global H3...
EPZ011989 is a potent, orally-available EZH2 inhibitor with robust in vivo activity. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenog...
EPZ005687 is a selective EZH2 enzyme inhibitor with Ki of 24 nM. It is 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyl...