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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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Images

Chemical Structure - EI1, EZH2 inhibitor (AB269817), expandable thumbnail

Key facts

CAS number
1418308-27-6
Form
Solid
Molecular weight
390.5 Da
Molecular formula
C23H26N4O2
PubChem identifier
72199293
Nature
Synthetic

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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.

Key facts

PubChem identifier
72199293
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

Storage

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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1 product image

  • Chemical Structure - EI1, EZH2 inhibitor (ab269817), expandable thumbnail

    Chemical Structure - EI1, EZH2 inhibitor (ab269817)

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

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Product protocols

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