2098621-17-9
2098621-17-9 结构式
基本信息
中文别名
化合物 T28999 英文别名
TPC-144[1,1':2',1''-Terphenyl]-4-carbonitrile, 5'-[[(3-endo)-3-amino-8-azabicyclo[3.2.1]oct-8-yl]carbonyl]-2'',3-difluoro-4''-(2-hydroxy-2-methylpropyl)-
应用领域
用途一
TPC-144 is a novel, 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.