GSK126

GSK126 is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases. (In Vitro) :GSK126 potently inhibits both wild-type and mutant EZH2 methyltransferase activity with similar potencies (Ki=0.5-3 nM) independent of substrate used, and is competitive with S-adenosyl-methionine (SAM) and non-competitive with peptide substrates. GSK126 is highly selective against other methyltransferases and multiple other protein classes (EZH1, IC50=680 nM) . Treatment of three SCLC cell lines with GSK126, induces growth inhibition. SCLC cell lines (Lu130, H209, and DMS53) are treated with 0.5, 2, and 8 μM GSK126, and growth curve is analyzed by WST-8 assay. Inhibition of cellular growth by GSK126 treatment is observed at 8 μM in all the three cell lines, while Lu130 and H209 are more sensitive to GSK126, even at lower doses. (In Vivo) :GSK126 is administered intraperitoneally at a dose volume of 0.2 mL per 20 g body weight in female beige SCID mice. GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice.

1346574-57-9

GSK2816126 | GSK-2816126 | GSK 2816126

>98% (HPLC)

DMSO: 3 mg/mL warmed (5.69 mM)

O=C (C1=CC (C2=CC=C (N3CCNCC3) N=C2) =CC4=C1C (C) =CN4[C@@H] (C) CC) NCC5=C (C) C=C (C) NC5=O

C31H38N6O2

526.67

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.