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≥98% (HPLC)

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GSK 503, GSK-503, N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide, 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
Empirical Formula (Hill Notation):
CAS Number:
Molecular Weight:
MDL number:

Quality Level


≥98% (HPLC)




white to beige


DMSO: 2 mg/mL, clear

storage temp.


Biochem/physiol Actions

GSK503 is a potent and selective histone-lysine N-methyltransferase EZH2 (ENX1, KMT6) inhibitor (IC50/Kiapp = 8/3 nM/EZH2, 27 nM/Y641C, <5 nM/A677G, Y641F/H/N/S EZH2 mutants vs. 633/636 nM/EZH1) with >4,000-fold selectivity over other histone methyltransferases and little potency toward panels of histone acetylases/deacetylases, kinases, GPCR/channels/transporters. GSK503 reduces splenocyte H3K27me3 level and prevents post immunization germinal center (GC) formation (150 mg/kg/day i.p.; mice) with good pharmacokinetics in vivo. GSK503 abrogates the GC hyperplasia phenotype of Ezh2(Y641N) mice and suppresses human DLBCL xenografts tumor growth in mice.

Storage Class

11 - Combustible Solids




Not applicable


Not applicable

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Michael D Onken et al.
Science signaling, 11(546) (2018-09-06)
Constitutively active G protein α subunits cause cancer, cholera, Sturge-Weber syndrome, and other disorders. Therapeutic intervention by targeted inhibition of constitutively active Gα subunits in these disorders has yet to be achieved. We found that constitutively active Gαq in uveal
Marc-Werner Dobenecker et al.
The Journal of experimental medicine, 215(4), 1101-1113 (2018-03-11)
Differentiation and activation of T cells require the activity of numerous histone lysine methyltransferases (HMT) that control the transcriptional T cell output. One of the most potent regulators of T cell differentiation is the HMT Ezh2. Ezh2 is a key
Loredana Puca et al.
Nature communications, 9(1), 2404-2404 (2018-06-21)
A major hurdle in the study of rare tumors is a lack of existing preclinical models. Neuroendocrine prostate cancer is an uncommon and aggressive histologic variant of prostate cancer that may arise de novo or as a mechanism of treatment
Wendy Béguelin et al.
Nature communications, 8(1), 877-877 (2017-10-14)
The EZH2 histone methyltransferase is required for B cells to form germinal centers (GC). Here we show that EZH2 mediates GC formation through repression of cyclin-dependent kinase inhibitor CDKN1A (p21Cip1). Deletion of Cdkn1a rescues the GC reaction in Ezh2 -/-
Daniel Zingg et al.
Cancer cell, 34(1), 69-84 (2018-07-17)
Human melanomas frequently harbor amplifications of EZH2. However, the contribution of EZH2 to melanoma formation has remained elusive. Taking advantage of murine melanoma models, we show that EZH2 drives tumorigenesis from benign BrafV600E- or NrasQ61K-expressing melanocytes by silencing of genes

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