Catalog No.: PC-26224Not For Human Use, Lab Use Only.
Soquelitinib (CPI-818) is a selective, covalent, orally bioavailable inhibitor of ITK kinase (Interleukin-2-inducible T cell kinase) with Kd of 6.5 nM, >80-fold selective over other TEC kinase family members, binds covalently to cysteine 442 of ITK and blocks its function.
Soquelitinib (CPI-818) is a selective, covalent, orally bioavailable inhibitor of ITK kinase (Interleukin-2-inducible T cell kinase) with Kd of 6.5 nM, >80-fold selective over other TEC kinase family members, binds covalently to cysteine 442 of ITK and blocks its function. Soquelitinib displays >100-fold selectivity compared to binding to resting lymphocyte kinase (RLK). Soquelitinib inhibits TCR signaling downstream of ITK and blocks IL-2 production, suppresses IL-2 secretion in Jurkat cells in response to TCR stimulation with a mean IC50 of 136 nM. Soquelitinib suppresses Th2 associated cytokines and induces Th1 skewing in CD4 T cells. Soquelitinib inhibits tumor growth and enhances cytolytic capacity of tumor infiltrating T cells. Soquelitinib enhances anti-PD1 and anti-CTLA4 efficacy in the CT26 tumor model. Soquelitinib inhibits T cell exhaustion process in vitro.
