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.
- UPC:
- 42172008
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- SML2718-25MG
- Product Size:
- 25/MG
- CAS:
- 1346572-63-1
