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EI1

A potent EZH2 inhibitor
Catalog #: B2270
SKU-Size Size Price Qty
B2270-5 5 mg
$125.00
B2270-25 25 mg
$475.00
More Sizes Get Quote

Product Details

Alternate Name 6-cyano-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-1-(1-ethylpropyl)-1H-indole-4-carboxamide
Appearance White solid
CAS # 1418308-27-6
Molecular Formula C₂₃H₂₆N₄O₂
Molecular Weight 390.5
Purity ≥98% by HPLC
Solubility DMSO (~2 mg/ml)
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
PubChem CID 72199293
Handling Protect from air and light
Storage Conditions -20°C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

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.


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