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AB218610

GSK343, histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor

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MW 541.7 Da, Purity >99%. Potent, selective, cell-permeable histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor. Inhibits EZH2 enzymatic activity (IC50 = 4 nM). Displays 60 fold selectivity for EZH2 over EZH1, and 1000 fold or greater selectivity against other histone methyltransferases. Inhibits H3K27 methylation in HCC1806 cells (IC50 < 200 nM).

View Alternative Names

AE (adipocyte enhancer) binding protein 2, AE-binding protein 2, AEBP2_HUMAN, Adipocyte enhancer-binding protein 2, CAF-1 subunit C, CAF-I 48 kDa subunit, CAF-I p48, CHET9, ChET 9 protein, Chromatin assembly factor 1 subunit C, Chromatin assembly factor I p48 subunit, Chromatin assembly factor/CAF 1 p48 subunit, Chromatin precipitated E2F target 9 protein, EED protein, EED, mouse, homolog of, EED_HUMAN, ENX-1, ENX-2, EZH1_HUMAN, EZH2_HUMAN, EZH2b, Embryonic ECTODERM development protein homolog, Embryonic ectoderm development, Embryonic ectoderm development isoform a, Embryonic ectoderm development protein, mouse, homolog of, Enhancer of zeste 2, Enhancer of zeste homolog 1, Enhancer of zeste homolog 1 (Drosophila), Enhancer of zeste homolog 2, Enhancer of zeste homolog 2 (Drosophila), Enhancer of zeste, Drosophila, homolog 2, Enx 1h, G1/S transition control protein binding protein RbAp46, Histone acetyltransferase type B subunit 2, Histone-binding protein RBBP4, Histone-binding protein RBBP7, Histone-lysine N-methyltransferase EZH1, Histone-lysine N-methyltransferase EZH2, JJAZ1, Joined to JAZF1 protein, KIAA0160, KMT 6, KMT6A, Lysine N-methyltransferase 6, MGC138867, MGC138868, MGC17922, MGC9169, MSI1 protein homolog, NURF55, Nucleosome-remodeling factor subunit RBAP46, Nucleosome-remodeling factor subunit RBAP48, OTTHUMP00000235483, OTTHUMP00000235484, OTTHUMP00000235485, Polycomb protein SUZ12, Polycomb protein eed, RB binding protein 4 chromatin remodeling factor, RBAP46, RBBP4_HUMAN, RBBP7_HUMAN, RbAp 48, Retinoblastoma-binding protein 4, Retinoblastoma-binding protein 7, Retinoblastoma-binding protein RbAp46, Retinoblastoma-binding protein p46, Retinoblastoma-binding protein p48, SUZ12 polycomb repressive complex 2 subunit, SUZ12_HUMAN, Suppressor of zeste 12 homolog, Suppressor of zeste 12 protein homolog, WAIT-1, WD protein associating with integrin cytoplasmic tails 1, WVS, WVS2, Zinc finger protein AEBP2, enhancer of zeste 2 polycomb repressive complex 2 subunit, hEED

Key facts

CAS number

1346704-33-3

Purity

>99%

Form

Solid

form

Molecular weight

541.7 Da

Molecular formula

C<sub>3</sub><sub>1</sub>H<sub>3</sub><sub>9</sub>N<sub>7</sub>O<sub>2</sub>

PubChem

71268957

Nature

Synthetic

Biochemical name

1-isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(2-(4-methylpiperazin-1-yl)pyridin-4-yl)-1H-indazole-4-carboxamide

Biological description

Potent, selective, cell-permeable histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor. Inhibits EZH2 enzymatic activity (IC50 = 4 nM). Displays 60 fold selectivity for EZH2 over EZH1, and 1000 fold or greater selectivity against other histone methyltransferases. Inhibits H3K27 methylation in HCC1806 cells (IC50 < 200 nM).

Canonical smiles

CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CC(=NC=C4)N5CCN(CC5)C)C(C)C

InChi

InChI=1S/C31H39N7O2/c1-6-7-23-14-21(4)35-31(40)26(23)18-33-30(39)25-15-24(16-28-27(25)19-34-38(28)20(2)3)22-8-9-32-29(17-22)37-12-10-36(5)11-13-37/h8-9,14-17,19-20H,6-7,10-13,18H2,1-5H3,(H,33,39)(H,35,40)

InChiKey

ULNXAWLQFZMIHX-UHFFFAOYSA-N

IUPAC Name

N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-propan-2-ylindazole-4-carboxamide

Product details

This product is manufactured by BioVision, an Abcam company and was previously called 2281 GSK343. 2281-5 is the same size as the 5 mg size of ab218610.

Properties and storage information

Shipped at conditions
Blue Ice
Appropriate long-term storage conditions
-20°C
Storage information
Store under desiccating conditions

Product protocols

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