TPC-144 is a potent and selective LSD1 inhibitor with a reversible inhibition mechanism that has antitumor activity in several human AML and SCLC cell lines and xenograft models. TPC-144 may provide clinical benefits and a favorable safety profile for the treatment of AML and SCLC patients. TPC-144 reversibly inhibited LSD1 in a histone peptide-competitive manner and did not form a covalent adduct with FAD. TPC-144 inhibited LSD1 with an IC50 of 1.5 nM and had selectivity over other histone demethylases and methyltransferases. TPC-144 induced cell differentiation, as indicated by derepression of hematopoietic transcription factor GFI1; increased expression of cell-surface markers such as CD86 and CD11b, and potently inhibited growth of AML cells (e.g., Kasumi-1, IC50 = 1.3 nM; MV4–11, IC50 = 2.4 nM; HEL, IC50 = 7.1 nM) by inducing apoptosis and cell cycle arrest. References:

纯度：≥98%

CAS：2098621-17-9