Src Inhibitor 3 is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. Src Inhibitor 3 shows the ability to increase T cell proliferation induced by T cell receptor signaling[1].
Src Inhibitor 3 reduces inhibitory LCK phosphorylation in vivo upon oral dosing and shows the ability to enhance T cell activation in response to antigen stimulation[1].
[1]. O'Malley DP, et al. Discovery of Pyridazinone and Pyrazolo[1,5-a]pyridine Inhibitors of C-Terminal Src Kinase. ACS Med Chem Lett. 2019 Sep 25;10(10):1486-1491.