Abcam, ab269817, EI1, EZH2 inhibitor

Size: 10mg / 25mg / 50mg / 100mg
MW 390.5 Da. Potent (IC 50 = 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
CAS number:1418308-27-6,
Form:SolidSee storage information,
Molecular weight:390.5 Da,
Molecular formula:C23H26N4O2,
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

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