A selective inhibitor of EZH2
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EI1

Item No. 19146

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-cyano-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-1-(1-ethylpropyl)-1H-indole-4-carboxamide
CAS Number
1418308-27-6
Molecular Formula
C23H26N4O2
Formula Weight
390.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 2 mg/ml
λmax
250, 309 nm
SMILES
O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C#N)=CC3=C2C=CN3C(CC)CC
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $178

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    10 mg

    $235

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    Product Description

    EI1 is an EZH2 inhibitor that has activity against both wild-type and Y641F mutant EZH2 (IC50s = 15 and 13 nM, respectively).1 It displays 90-fold selectivity for EZH2 over EZH1 and >10,000-fold over other lysine methyltransferases. EI1 blocks cellular H3K27 methylation and activates PRC2-specific gene expression.1 Inhibition of EZH2 by EI1 in diffused large B cell lymphoma cells carrying Y641 mutations results in decreased proliferation, cell cycle arrest, and apoptosis.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Qi, W., Chan, H.M., Teng, L., et al. Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation. Proc. Natl. Acad. Sci. USA 109(52), 21360-21365 (2012).