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.
MedKoo Cat#: 407814
Name: TPC-144
CAS#: 2098621-17-9
Chemical Formula: C31H31F2N3O2
Exact Mass: 515.2384
Molecular Weight: 515.60
Elemental Analysis: C, 72.21; H, 6.06; F, 7.37; N, 8.15; O, 6.21
The following data is based on the product molecular weight 515.60 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
