GSK-114

Research use only, not for human use.

GSK-114 is a potent, selective TNNI3K inhibitor with IC50 of 25 nM.

GSK-114 is a potent, selective TNNI3K inhibitor with IC50 of 25 nM, dispalys 40-fold over B-Raf, exceptional broad spectrum kinase selectivity (IC50>1,000 nM, 99% of kinases, 291/294); has adequate oral exposure to enable its use in cellular and in vivo studies.

At a concentration of 1 μM, GSK114 demonstrated an affinity for seven other kinases: ACK1, B-Raf, GAK, MEK5, PDGFRB, STK36, and ZAK.

GSK-114 affords the best balance of specificity and pharmacokinetics, demonstrating useful oral exposure (poDNAUC=0.18, Cmax=130 ng/ml @ 2 mg/kg, t1/2=3.6 hr, rat Fu=20.2%).

GSK114

MAPK/ERK Signaling

MEK

MEK

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1301761-96-5

417.484

C19H23N5O4S

>98% (HPLC)

In Vitro:?DMSO : 5.95 mg/mL (14.25 mM)

O=S(C1=CC=C(N(C)C)C(NC2=C3C=C(OC)C(OC)=CC3=NC=N2)=C1)(NC)=O

3-((6,7-dimethoxyquinazolin-4-yl)amino)-4-(dimethylamino)-N-methylbenzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years