1396772-26-1 Usage
Description
1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide, also known as EPZ005687, is a potent and selective inhibitor of the lysine methyltransferase EZH2. It acts competitively with the EZH2 substrate S-adenosylmethionine and has greater than 500-fold selectivity against 15 other protein methyltransferases. EPZ005687 blocks trimethylation of the PRC2 target histone 3 lysine 27, which plays a crucial role in the regulation of gene expression.
Uses
Used in Pharmaceutical Industry:
EPZ005687 is used as a potent and selective inhibitor of EZH2 for the treatment of various types of cancer. It has shown to decrease the proliferation of lymphoma cells carrying mutant EZH2, making it a promising therapeutic agent for cancer patients with specific genetic mutations.
Used in Research Applications:
In the field of research, EPZ005687 is utilized as a tool to study the role of EZH2 in gene regulation and its involvement in the development and progression of cancer. It helps researchers understand the underlying mechanisms of EZH2-mediated processes and identify potential therapeutic targets for cancer treatment.
Used in Drug Development:
EPZ005687 serves as a lead compound in the development of new drugs targeting EZH2 for cancer therapy. Its high selectivity and potency make it an attractive candidate for further optimization and development into more effective and safer drugs for cancer patients.
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.
