T338C Src-IN-2 

T338C Src-IN-2 is a mutant c-Src kinase inhibitor, with an IC₅₀ of 317 nM against T338C c-Src, 57 nM against T338C/V323A c-Src, and 19 nM against T338C/V323S c-Src. T338C Src-IN-2 inhibits the kinase activity of endogenous cysteine gatekeeper MOK. T338C Src-IN-2 reduces global phosphotyrosine levels in v-Src-ES1-transformed NIH-3T3 cells^[1].

T338C Src-IN-2 (Compound 13) (1 μM) potently inhibits immunoprecipitated MOK at a concentration of 1 μM, reducing kinase activity to near-background levels^[1].
T338C Src-IN-2 (0-10 μM; 1 h) selectively inhibits v-Src-ES1 (v-Src^I338C) in NIH-3T3 cells in a dose-dependent manner in vitro, and shows no activity against v-Src^I338T at concentrations up to 10 μM^[1].
T338C Src-IN-2 (10 min) exhibits enhanced potency against the double mutants c-Src-ES2^T338C/V323A and c-Src-ES3^T338C/V323S, with IC₅₀ values of 57 nM and 19 nM, respectively, representing 6-fold and 17-fold increases in activity compared to that against c-Src-ES1^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

327.36

C₁₇H₁₈FN₅O

1351927-00-8

Solid

White to off-white

NC1=C2C(N(C(C)C)N=C2CC3=CC(C(CF)=O)=CC=C3)=NC=N1

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

• [1]. Garske AL, et al. Chemical genetic strategy for targeting protein kinases based on covalent complementarity. Proc Natl Acad Sci U S A. 2011;108(37):15046-15052.  [Content Brief]