[CAS NO. 1346572-63-1] GSK503

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PRODUCTS SPECIFICATIONS [1346572-63-1]

Catalog

SLK-S7804

Brand

Selleck

CAS

1346572-63-1

DESCRIPTION [1346572-63-1]

Overview

MDL	MFCD28405142
Molecular Weight	526.67
Molecular Formula	C31H38N6O2
SMILES	O=C(C1=CC(C2=CC=C(N3CCN(C)CC3)N=C2)=CC4=C1C(C)=CN4C(C)C)NCC5=C(C)C=C(C)NC5=O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.8987 mL	9.4936 mL	18.9872 mL
5 mM	0.3797 mL	1.8987 mL	3.7974 mL
10 mM	0.1899 mL	0.9494 mL	1.8987 mL
50 mM	0.0380 mL	0.1899 mL	0.3797 mL

Description

GSK503 is a potent and specific methyltransferase inhibitor.

Targets

EZH2 ^[1]

8 nM

In vitro

GSK503 inhibits the methyltransferase activity of WT and mutant EZH2 with similar potency. In a panel of seven DLBCL cell lines, GSK503 causes growth inhibition and the effects are enhanced by ABT737 or Obatoclax.

In vivo

In C57BL6 mice immunized with SRBC, GSK503 (150 mg/kg, i.p.) reduced the level of H3K27me3 in splenocytes. In male SCID mice bearing SUDHL4 and SUDHL6 tumors, GSK503 (150 mg/kg, i.p.) inhibits tumor growth. In C57Bl/6 mice bearing murine B16-F10 tumors, GSK503 (150 mg/kg, i.p.) significantly reduces global H3K27me3 levels, inhibits tumor growth and virtually abolishes metastases formation.

References

[1] Béguelin W, et al. Cancer Cell. 2013, 23(5), 677-692
[2] Zingg D, et al. Nat Commun. 2015, 6, 6051.