SB-747651A dihydrochloride (SB747651A) is a potent, specific and ATP-competitive inhibitor of MSK1 (mitogen- and stress-activated kinase 1) with IC50 of 11 nM.
SB-747651A dihydrochloride (SB747651A) is a potent, specific and ATP-competitive inhibitor of MSK1 (mitogen- and stress-activated kinase 1) with IC50 of 11 nM. SB-747651A inhibits four other kinases, PRK2 (double-stranded-RNA-dependent protein kinase 2), RSK1 (ribosomal S6 kinase 1), p70S6K (S6K is S6 kinase) (p70RSK) and ROCK-II (Rho-associated protein kinase 2), with a similar potency to MSK1 against a panel of 117 protein kinases. SB-747651A fully inhibits MSK1/2 activity at 5-10 μM in cells. SB-747651A inhibits the production of the anti-inflammatory cytokine IL-10 in wild-type, but not MSK1/2-knockout, macrophages following LPS (lipopolysaccharide) stimulation. SB-747651A reduced cell proliferation, spheroid formation, migration and chemoresistance in patient-derived glioblastoma spheroid cultures and a murine orthotopic xenograft model.
