TETi76

**TETi76** is a synthetic small molecule and orally active inhibitor of the TET family of DNA dioxygenases (TET1, TET2, TET3), with IC50 values of 1.5 μM, 9.4 μM, and 8.8 μM, respectively. It mimics and amplifies the effects of 2-hydroxyglutarate (2HG) to suppress residual TET enzymatic activity in TET2-mutant cells, which rely on TET1 and TET3 for survival, thereby selectively inducing apoptosis in mutant leukemia cells while sparing normal hematopoietic stem and progenitor cells. Developed by researchers at the Cleveland Clinic’s Taussig Cancer Institute and Lerner Research Institute, led by Drs. Jaroslaw Maciejewski and Babal Kant Jha with chemistry support from Dr. James Phillips, it shows preclinical efficacy in suppressing clonal evolution in clonal hematopoiesis of indeterminate potential (CHIP) and TET2-mutant myeloid leukemia models, including xenografts, positioning it as a potential targeted therapy for TET2-driven hematological malignancies.

Other names

TETi76 esterTETi-76 esterTETi 76 ester