1598383-40-4 Usage
Description
The lysine methyltransferase EZH2 (KMT6), part of polycomb repressive complex 2, catalyzes trimethylation of lysine 27 on histone H3 and is involved in proliferation and aggressive cell growth associated with neoplastic cells. EPZ011989 is an orally bioavailable EZH2 inhibitor with Ki values that are less than 3 nM for wild type and Tyr646 mutated EZH2. It displays 15-fold selectivity for EZH2 over EZH1 and is without effect against an array of other lysine methyltransferases. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.
Uses
N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-[ethyl[trans-4-[(2-methoxyethyl)methylamino]cyclohexyl]amino]-2-methyl-5-[3-(4-morpholinyl)-1-propyn-1-yl]-benzamide is used in biological studies as inhibitors of EZH2 histone methyltransferase for the treatment of cancer.
Check Digit Verification of cas no
The CAS Registry Mumber 1598383-40-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,5,9,8,3,8 and 3 respectively; the second part has 2 digits, 4 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 1598383-40:
(9*1)+(8*5)+(7*9)+(6*8)+(5*3)+(4*8)+(3*3)+(2*4)+(1*0)=224
224 % 10 = 4
So 1598383-40-4 is a valid CAS Registry Number.
1598383-40-4Relevant articles and documents
EPZ011989, A potent, orally-available EZH2 inhibitor with robust in vivo activity
Campbell, John E.,Kuntz, Kevin W.,Knutson, Sarah K.,Warholic, Natalie M.,Keilhack, Heike,Wigle, Tim J.,Raimondi, Alejandra,Klaus, Christine R.,Rioux, Nathalie,Yokoi, Akira,Kawano, Satoshi,Minoshima, Yukinori,Choi, Hyeong-Wook,Porter Scott, Margaret,Waters, Nigel J.,Smith, Jesse J.,Chesworth, Richard,Moyer, Mikel P.,Copeland, Robert A.
, p. 491 - 495 (2015/05/27)
Inhibitors of the protein methyltransferase Enhancer of Zeste Homolog 2 (EZH2) may have significant therapeutic potential for the treatment of B cell lymphomas and other cancer indications. The ability of the scientific community to explore fully the spectrum of EZH2-associated pathobiology has been hampered by the lack of in vivo-active tool compounds for this enzyme. Here we report the discovery and characterization of EPZ011989, a potent, selective, orally bioavailable inhibitor of EZH2 with useful pharmacokinetic properties. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma. Hence, this compound represents a powerful tool for the expanded exploration of EZH2 activity in biology.