EI1 | B2270

EI1 is a potent EZH2 inhibitor that has activity against both wild-type and Y641F mutant EZH2 (IC₅₀s = 15 and 13 nM, respectively). It displays 90-fold selectivity for EZH2 over EZH1 and >10,000-fold selectivity over other lysine methyltransferases. EI1 blocks cellular H3K27 methylation and activates PRC2-specific gene expression. Inhibition of EZH2 by EI1 in diffused large B cell lymphoma cells carrying Y641 mutations results in decreased proliferation, cell cycle arrest, and apoptosis.

EI1 is a potent EZH2 inhibitor that has activity against both wild-type and Y641F mutant EZH2 (IC₅₀s = 15 and 13 nM, respectively). It displays 90-fold selectivity for EZH2 over EZH1 and >10,000-fold selectivity over other lysine methyltransferases. EI1 blocks cellular H3K27 methylation and activates PRC2-specific gene expression. Inhibition of EZH2 by EI1 in diffused large B cell lymphoma cells carrying Y641 mutations results in decreased proliferation, cell cycle arrest, and apoptosis.

B2270 | EI1 DataSheet

Alternate Name/Synonyms: 6-cyano-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-1-(1-ethylpropyl)-1H-indole-4-carboxamide

Appearance: White solid

Formulation: N/A

CAS Number: 1418308-27-6

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₃H₂₆N₄O₂

Molecular Weight: 390.5

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO (~2 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent EZH2 inhibitor

MDL Number: N/A

PubChem CID: 72199293

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)

InChi Key: PFHDWRIVDDIFRP-UHFFFAOYSA-N