A dual inhibitor of BRD4 and HDAC1
| Cas No. | 2614417-90-0 |
| Canonical SMILES | CC1=C(C)C(C(C2=CC=C(Cl)C=C2)=N[C@H]3CC(NC4=CC=C(C(NC5=C(N)C=CC=C5)=O)C=C4)=O)=C(S1)N6C3=NN=C6C |
| 分子式 | C32H28ClN7O2S |
| 分子量 | 610.1 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 10 mg/ml |
| 储存条件 | -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 µM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 µM) and for HDAC1 over HDAC2 (IC50= 2.5 µM). TW9 (50 nM) induces apoptosis in, and inhibits proliferation of, MIA PaCa-2 pancreatic cancer cells. It induces cell cycle arrest at the G1phase in HPAC pancreatic cancer cells when used at a concentration of 2 µM. TW9 acts synergistically with gemcitabine to reduce the viability of HPAC cells. 1.Zhang, X., Zegar, T., Weiser, T., et al.Characterization of a dual BET/HDAC inhibitor for treatment of pancreatic ductal adenocarcinomaInt. J. Cancer147(10)2847-2861(2020) |
