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Merck

SML2718

GSK503

≥98% (HPLC)

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C31H38N6O2
CAS Number:
1346572-63-1
Molecular Weight:
526.67
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD28405142

Key Documents

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Product Name

GSK503, ≥98% (HPLC)

SMILES string

[nH]1[c](c(c(cc1C)C)CNC(=O)c2c3c([n](cc3C)C(C)C)cc(c2)c4cnc(cc4)N5CCN(CC5)C)=O

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

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

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.
Potent and selective histone-lysine N-methyltransferase EZH2 (ENX1, KMT6) inhibitor in vitro and in vivo. Displays >200-fold selectivity over EZH1.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Jinfeng Cao et al.
The Journal of pathology, 245(4), 433-444 (2018-05-08)
Malignant melanoma of the conjunctiva (CM) is an uncommon but potentially deadly disorder. Many malignancies show an increased activity of the epigenetic modifier enhancer of zeste homolog 2 (EZH2). We studied whether EZH2 is expressed in CM, and whether it
Rosa Martin-Mateos et al.
Cellular and molecular gastroenterology and hepatology, 7(1), 197-209 (2018-12-13)
Transdifferentiation of hepatic stellate cells (HSCs) into myofibroblasts is a key event in the pathogenesis of liver fibrosis. Transforming growth factor β (TGF-β) and platelet-derived growth factor (PDGF) are canonical HSC activators after liver injury. The aim of this study
Guanghui Hu et al.
Oncotarget, 8(35), 58654-58667 (2017-09-25)
The long noncoding RNA HOTAIR promotes the development and progression of several tumors. Here, the clinical significance and role of HOTAIR in renal cell carcinoma (RCC) tumorigenesis were explored. The results showed that increased expression of HOTAIR predicted a poor
Wendy Béguelin et al.
Cancer cell, 23(5), 677-692 (2013-05-18)
The EZH2 histone methyltransferase is highly expressed in germinal center (GC) B cells and targeted by somatic mutations in B cell lymphomas. Here, we find that EZH2 deletion or pharmacologic inhibition suppresses GC formation and functions. EZH2 represses proliferation checkpoint
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
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