TPC-144

CAS NO.：2098621-17-9
Empirical Formula: C31H31F2N3O2
Molecular Weight: 515.59
Update Date: 2026-05-11 16:31:51

What is TPC-144?

Description

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.

Properties of TPC-144

Boiling point:	665.5±55.0 °C(Predicted)
Density	1.32±0.1 g/cm3(Predicted)
pka	14.25±0.29(Predicted)

Safety information for TPC-144

Computed Descriptors for TPC-144

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