TETi76 is an orally active TET family inhibitor with IC50 values of 1.5, 9.4 and 8.8 μM for TET1, TET2 and TET3, respectively. TETi76 competitively binds to the active site of TET enzymes, reduces cytosine droxymetlation and restricts clonal growth of TET2 mutants in vitro and in vivo, but does not affect the growth of normal hematopoietic precursor cells. TETi76 can be used for leukemia research.
References:
[1]. Yihong Guan, et al. A therapeutic strategy for preferential targeting of TET2-mutant and TET dioxygenase–deficient cells in myeloid neoplasms. Blood cancer discovery 2.2 (2021): 146-161.