A potent, selective inhibitor of EZH2
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EPZ005687

Item No. 13966

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-cyclopentyl-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[4-(4-morpholinylmethyl)phenyl]-1H-indazole-4-carboxamide
CAS Number
1396772-26-1
Molecular Formula
C32H37N5O3
Formula Weight
539.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml
λmax
259, 312 nm
SMILES
O=C(NCC1=C(C)C=C(C)NC1=O)C2=CC(C3=CC=C(CN4CCOCC4)C=C3)=CC5=C2C=NN5C6CCCC6
InChi Code
InChI=1S/C32H37N5O3/c1-21-15-22(2)35-32(39)28(21)18-33-31(38)27-16-25(17-30-29(27)19-34-37(30)26-5-3-4-6-26)24-9-7-23(8-10-24)20-36-11-13-40-14-12-36/h7-10,15-17,19,26H,3-6,11-14,18,20H2,1-2H3,(H,33,38)(H,35,39)
InChi Key
ZOIBZSZLMJDVDQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $95

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    10 mg

    $168

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    25 mg

    $370

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    50 mg

    $647

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    Cayman Chemical
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    Product Description

    EPZ005687 is a potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 24 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2).1 It acts competitively with the EZH2 substrate S-adenosylmethionine.1,2,3 EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against EZH1.1 It blocks trimethylation of the PRC2 target histone 3 lysine 27 (IC50 = 80 nM), decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Knutson, S.K., Wigle, T.J., Warholic, N.M., et al. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat. Chem. Biol. 8(11), 890-896 (2012).

    2. Wigle, T.J., and Copeland, R.A. Drugging the human methylome: An emerging modality for reversible control of aberrant gene transcription. Curr. Opin. Chem. Biol. 17(3), 369-378 (2013).

    3. Konze, K.D., Ma, A., Li, F., et al. An orally bioavailable chemical probe of the lysine methyltransferases EZH2 and EZH1. ACS Chem. Biol. 8(6), 1324-1334 (2013).