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Alternative_name
6-cyano-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-1-(1-ethylpropyl)-1H-indole-4-carboxamide
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Description
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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CAS Number
1418308-27-6
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Structure Available
Yes
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Salt Form
No
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Molecular Formula
C₂₃H₂₆N₄O₂
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Molecular Weight
390.5
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Cell Permeable
Yes
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Purity
≥98% by HPLC
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Solubilities
DMSO (~2 mg/ml)
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Handling
Protect from air and light
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Tag Line
A potent EZH2 inhibitor
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Storage Condition
-20°C
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Shipping Condition
gel pack
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Shelf Life
36 months
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PubChem CID
72199293
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SMILES
CCC(CC)N1C=CC2=C(C=C(C=C21)C#N)C(=O)NCC3=C(C=C(NC3=O)C)C
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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)
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InChi Key
PFHDWRIVDDIFRP-UHFFFAOYSA-N
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MSDS Available
YES