| Identification | Back Directory | [Name]
TPC-144 | [CAS]
2098621-17-9 | [Synonyms]
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)- | [Molecular Formula]
C31H31F2N3O2 | [MOL File]
2098621-17-9.mol | [Molecular Weight]
515.6 |
| Hazard Information | Back Directory | [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. |
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| Company Name: |
BOC Sciences
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| Tel: |
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| Website: |
https://www.bocsci.com |
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