A selective, cell-permeable EZH2 inhibitor
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GSK343

Item No. 14094

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)Epigenetic Chemical Probe Guide (PDF)
Technical Information
Formal Name
N-[(1,2-dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indazole-4-carboxamide
CAS Number
1346704-33-3
Molecular Formula
C31H39N7O2
Formula Weight
541.7
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 1 mg/mlEthanol: 2 mg/ml
λmax
256, 305 nm
SMILES
CC(C)N(N=C1)C2=C1C(C(NCC3=C(CCC)C=C(C)NC3=O)=O)=CC(C4=CC(N5CCN(C)CC5)=NC=C4)=C2
InChi Code
InChI=1S/C31H39N7O2/c1-6-7-23-14-21(4)35-31(40)26(23)18-33-30(39)25-15-24(16-28-27(25)19-34-38(28)20(2)3)22-8-9-32-29(17-22)37-12-10-36(5)11-13-37/h8-9,14-17,19-20H,6-7,10-13,18H2,1-5H3,(H,33,39)(H,35,40)
InChi Key
ULNXAWLQFZMIHX-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

    $128

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    10 mg

    $178

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    25 mg

    $341

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    Cayman Chemical
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    Product Description

    The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.1 GSK343 is a cell-permeable EZH2 inhibitor (IC50 = 4 nM) that is 60-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases.2 GSK343 has been shown to inhibit the trimethylation of H3K27 in HCC1806 cells with an IC50 value of 174 nM.2 See Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Simon, J.A., and Lange, C.A. Roles of the EZH2 histone methyltransferase in cancer epigenetics. Mutat. Res. 647(1-2), 21-29 (2008).

    2. Verma, S.K., Tian, X., LaFrance, L.V., et al. Identification of potent, selective, cell-active inhibitors of the histone lysine methyltransferase EZH2. ACS Med. Chem. Lett. 3(12), 1091-1096 (2012).