TPST2-IN-1

TPST2-IN-1 is a potent and selective TPST2 inhibitor, with an IC50 of 946 nM and a Ka of 19.4 μM. It functions by inhibiting TPST2 activity, thereby increasing the phosphorylation level of Stat1 and upregulating the expression of the IFNγ-responsive gene CXCL10. Exhibiting antitumor activity, TPST2-IN-1 enhances T cell-mediated antitumor immunity, characterized by increased infiltration of effector CD8+ T cells. This compound is applicable in cancer research, such as studies involving colorectal cancer.