1396772-26-1 Usage
Uses
Different sources of media describe the Uses of 1396772-26-1 differently. You can refer to the following data:
1. EPZ005687 is a potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 24 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2). It acts competitively with the EZH2 substrate S-adenosylmethionine. EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against EZH1. It blocks trimethylation of the PRC2 target histone 3 lysine 27 (IC50 = 80 nM), decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2.[Cayman Chemical]
2. EPZ005687 is a potent and selective inhibitor of EZH2.
Biological Activity
epz005687 is a potent inhibitor of ezh2, an enzymatic subunit of polycomb repressive complex 2 (prc2) catalyzing the methylation of histone h3 lysine 27 (h3k27), that inhibits ezh2 with a value of inhibition constant ki of 24 nm, which is 500-fold and 50-fold greater in selectivity than 15 other protein methyltransferases and closely related ezh1 respectively. epz005687 concentration-dependently inhibits the enzymatic activity of prc2 with a value of 50% inhibition concentration ic50 of 54 nm through binding to the s-adenosylmethionine (sam) pocket of the ezh2 set domain. study results have shown that epz005687 reduces h3k27 methylation in a variety of lymphoma cells and induces apoptotic cell killing in heterozygous tyr641 or ala677 mutant cells.knutson sk, wigle tj, warholic nm, sneeringer cj, allain cj, klaus cr, sacks jd, raimondi a, majer cr, song j, scott mp, jin l, smith jj, olhava ej, chesworth r, moyer mp, richon vm, copeland ra, keilhack h, pollock rm, kuntz kw. a selective inhibitor of ezh2 blocks h3k27 methylation and kills mutant lymphoma cells. nat chem biol. 2012 nov;8(11):890-6.
Check Digit Verification of cas no
The CAS Registry Mumber 1396772-26-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,9,6,7,7 and 2 respectively; the second part has 2 digits, 2 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1396772-26:
(9*1)+(8*3)+(7*9)+(6*6)+(5*7)+(4*7)+(3*2)+(2*2)+(1*6)=211
211 % 10 = 1
So 1396772-26-1 is a valid CAS Registry Number.
1396772-26-1Relevant articles and documents
SUBSTITUTED 6,5-FUSED BICYCLIC HETEROARYL COMPOUNDS
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, (2012/09/21)
The present invention relates to substituted 6,5 -fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.
