A potent, selective EZH2 inhibitor
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Isomer(s)
15415GSK126
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GSK503

Item No. 18531

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-(1-methylethyl)-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide
CAS Number
1346572-63-1
Molecular Formula
C31H38N6O2
Formula Weight
526.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mLDMF:PBS(pH 7.2)(1:1): 0.5 mg/mLDMSO: 15 mg/mLEthanol: 2 mg/ML
λmax
235, 282 nm
SMILES
CN1CCN(C2=NC=C(C3=CC(C(NCC4=C(C)C=C(C)NC4=O)=O)=C(C(C)=CN5C(C)C)C5=C3)C=C2)CC1
InChi Code
InChI=1S/C31H38N6O2/c1-19(2)37-18-21(4)29-25(30(38)33-17-26-20(3)13-22(5)34-31(26)39)14-24(15-27(29)37)23-7-8-28(32-16-23)36-11-9-35(6)10-12-36/h7-8,13-16,18-19H,9-12,17H2,1-6H3,(H,33,38)(H,34,39)
InChi Key
HRDQQHUKUIKFHT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

    $154

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    25 mg

    $337

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    Cayman Chemical
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    Product Description

    GSK503 is an inhibitor of EZH2 that prevents the methyltransferase activity of wild-type and mutant EZH2 with similar potency (apparent Ki = 3-27 nM).1 It is more than 200-fold selective for EZH2 over EZH1 and more than 4,000-fold selective over other histone methyltransferases. GSK503 displays favorable pharmacokinetics in mice. It prevents germinal center formation and hyperplasia that is relevant to lymphoma generation and inhibits growth and metastasis of cutaneous melanomas in mice.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Béguelin, W., Popovic, R., Teater, M., et al. EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation. Cancer Cell. 23(5), 677-692 (2013).

    2. Zingg, D., Debbache, J., Schaefer, S.M., et al. The epigenetic modifier EZH2 controls melanoma growth and metastasis through silencing of distinct tumour suppressors. Nat. Commun. 6, (2015).