ChemicalBook Produktkatalog Bio- und Chemieingenieurwesen Inhibitoren Epigenetik Histon-Methyltransferase-Inhibitoren 1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide

1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide Struktur

1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide

Bezeichnung:1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide

CAS-Nr1396772-26-1

Englisch Name:1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide

CBNumberCB02645672

SummenformelC32H37N5O3

Molgewicht539.67

MOL-Datei1396772-26-1.mol

1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide physikalisch-chemischer Eigenschaften

Siedepunkt	797.9±60.0 °C(Predicted)
Dichte	1.31±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	insoluble in EtOH; insoluble in H2O; ≥3.86 mg/mL in DMSO
Aggregatzustand	solid
pka	11.88±0.10(Predicted)
Farbe	Off-white to yellow

Gefahreninformationscode (GHS)

1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
EPZ005687 is a potent and selective inhibitor of EZH2.
Verwenden
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]
Definition
ChEBI: 1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(4-morpholinylmethyl)phenyl]-4-indazolecarboxamide is a member of indazoles.
Biologische Aktivität
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.
target
EZH2

1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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