Src Inhibitor 1 (Src Kinase Inhibitor 1) is a potent and selective dual site Src tyrosine kinase inhibitor.

Lck:88nM, Src:44 nM

Src-I1在激酶的ATP和肽结合位点具有竞争性作用。其IC50值对Src和Lck分别为44 nM和88 nM[1]。Src-I1是一种强效的Src抑制剂（IC50=0.18 μM），同时也能以类似Src的效力抑制Src家族的其他成员。此外，它对CHK2的抑制效力与对Src相当，而对Aurora B的抑制效力略低[2]。

Assays (25.5 μL volume) are carried out robotically at room temperature (21°C) and are linear with respect to time and enzyme concentration under the conditions used. Assays are performed for 30 min using Multidrop Micro reagent dispensers in a 96-well format. The concentration of magnesium acetate in the assays is 10 mM and [γ-33P]ATP (800 c.p.m./pmol) is used at 5, 20 or 50 μM as indicated, in order to be at or below the Kmfor ATP for each enzyme.The assays are initiated with MgATP, stopped by the addition of 5 μL of 0.5 M orthophosphoric acid and spotted on to P81 filter plates using a unifilter harvester. The IC50 values of inhibitors are determined after carrying out assays at ten different concentrations of each compound[2].