T-3775440 hydrochloride 是一种不可逆的赖氨酸特异性组蛋白去甲基化酶 (LSD1) 抑制剂，IC50值为 2.1 nM。

T-3775440 hydrochloride is an irreversible inhibitor of lysine-specific histone demethylase (LSD1)(IC50 : 2.1 nM).

T-3775440, a novel irreversible LSD1 inhibitor.?Cell growth analysis of leukemia cell lines revealed that acute erythroid leukemia (AEL) and acute megakaryoblastic leukemia cells (AMKL) were highly sensitive to this compound.?T-3775440 treatment enforced transdifferentiation of erythroid/megakaryocytic lineages into granulomonocytic-like lineage cells.?Mechanistically, T-3775440 disrupted the interaction between LSD1 and growth factor-independent 1B (GFI1B), a transcription factor critical for the differentiation processes of erythroid and megakaryocytic lineage cells.?Knockdown of LSD1 and GFI1B recapitulated T-3775440-induced transdifferentiation and cell growth suppression, highlighting the significance of LSD1-GFI1B axis inhibition with regard to the anti-AML effects of T-3775440[1].

T-3775440 exhibited significant antitumor efficacy in AEL and AMKL xenograft models[1].

1422535-52-1

C18H23ClN4O

346.85

DMSO:30.18 mg/mL (87.01 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years