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AB269817

EI1, EZH2 inhibitor

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MW 390.5 Da. Potent (IC50 = 15 nM for wild-type enzyme; 13 nM for Y641F mutant enzyme) EZH2 inhibitor. Selective versus EZH1 (142-fold). Highly selective (>10,000-fold) against a panel of 10 other human methyltransferases. Inhibits cellular H3K27 methylation and activates Ezh2 target gene p16 expression in diffuse large B-cell lymphoma cells (DLBLC). Selectively inhibits growth and promotes cell cycle arrest and apoptosis of DLBLC cells with Y641 EZH2 mutations.
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Chemical Structure - EI1, EZH2 inhibitor (AB269817)
  • Chemical Structure

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Chemical Structure - EI1, EZH2 inhibitor (AB269817)

Chemical structure of EI1, EZH2 inhibitor, 1418308-27-6

Key facts

CAS number

1418308-27-6

Form

Solid

form

Molecular weight

390.5 Da

Molecular formula

C<sub>2</sub><sub>3</sub>H<sub>2</sub><sub>6</sub>N<sub>4</sub>O<sub>2</sub>

PubChem

72199293

Nature

Synthetic

Solubility

Soluble in DMSO to 50 mM

Biochemical name

6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide

Biological description

Potent (IC50 = 15 nM for wild-type enzyme; 13 nM for Y641F mutant enzyme) EZH2 inhibitor. Selective versus EZH1 (142-fold). Highly selective (>10,000-fold) against a panel of 10 other human methyltransferases. Inhibits cellular H3K27 methylation and activates Ezh2 target gene p16 expression in diffuse large B-cell lymphoma cells (DLBLC). Selectively inhibits growth and promotes cell cycle arrest and apoptosis of DLBLC cells with Y641 EZH2 mutations.

Canonical smiles

CCC(CC)N1C=CC2=C(C=C(C=C21)C#N)C(=O)NCC3=C(C=C(NC3=O)C)C

InChi

InChI=1S/C23H26N4O2/c1-5-17(6-2)27-8-7-18-19(10-16(12-24)11-21(18)27)22(28)25-13-20-14(3)9-15(4)26-23(20)29/h7-11,17H,5-6,13H2,1-4H3,(H,25,28)(H,26,29)

InChiKey

PFHDWRIVDDIFRP-UHFFFAOYSA-N

IUPAC Name

6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide

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Complementary Products

Biochemicals

AB269816

GSK126, EZH2 methyltransferase inhibitor

Chemical Structure - GSK126, EZH2 methyltransferase inhibitor (AB269816)

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Biochemicals

AB146152

UNC1999, EZH2 methyltransferase inhibitor

Chemical Structure - UNC1999, EZH2 methyltransferase inhibitor (AB146152)

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Proteins & Peptides

AB156723

Recombinant Human EED protein

SDS-PAGE - Recombinant Human EED protein (AB156723)

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Proteins & Peptides

AB271504

Recombinant human RBBP4 + EED + SUZ12 + AEBP2 + EZH2 (mutated P132S) protein (Active)

Functional Studies - Recombinant human RBBP4 + EED + SUZ12 + AEBP2 + EZH2 (mutated P132S) protein (Active) (AB271504)

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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
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Product protocols

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