TPC-144
- CAS No.
- 2098621-17-9
- Chemical Name:
- TPC-144
- 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)-
- CBNumber:
- CB34920750
- Molecular Formula:
- C31H31F2N3O2
- Molecular Weight:
- 515.6
- MDL Number:
- MOL File:
- 2098621-17-9.mol
TPC-144 Chemical Properties,Uses,Production
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.
TPC-144 Preparation Products And Raw materials
Raw materials
Preparation Products
TPC-144 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38631 | 58 | |
| TargetMol Chemicals Inc. | +8613564774135 | zijue.cai@tsbiochem.com | United States | 19881 | 58 |
| BOC Sciences | -- | info@bocsci.com | USA | 0 | 65 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 19699 | 58 |
| Supplier | Advantage |
|---|---|
| TargetMol Chemicals Inc. | 58 |
| TargetMol Chemicals Inc. | 58 |
| BOC Sciences | 65 |
| TargetMol Chemicals Inc. | 58 |
