半岛bd体育手机客户端 说明
生化/生理作用
IACS-9571 is a dimethylamine analogue.
IACS-9571 is a high-affinity, potent TRIM24/BRPF1 bromodomain (BrD) inhibitor (Kd = 1.3/2.1 nM by DiscoveRx) with good selectivity over other BrDs (BRPF2/3 Kd = 12/27 nM, BAZ2B/TAF1 BrD2/BRD4 BrD1,2 Kd = 0.4/1.8/>10 μM by DiscoveRx; ≤63% binding inhibition of 25 other BrDs at 1 μM). IACS-9571 potently blocks H3K23Ac peptide from TRIM24 BrD binding (IC50 = 7.6 nM) and displaces ectopically expressed TRIM24 PHD-BrD from endogenous histone H3 in 2-hr 5 μM SAHA-stimulated HeLa cells (IC50 = 50 nM). When adiministered in mice, IACS-9571 exhibits good pharmacokinetics and oral availabilityin vivo(F = 29%, 10 mg/kg p.o.).
基本信息
| 经验(实验)分子式 | C32H42N4O8S · CF3CO2H |
| 分子量 | 756.79 |
半岛bd体育手机客户端 性质
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 颜色 | white to beige |
| 溶解性 | DMSO: 2 mg/mL, clear |
| 储存温度 | 2-8℃ |
| SMILES string | O=S(C1=CC=C(C(OC)=C1)OC)(NC2=C(C=C(C3=C2)N(C(N3C)=O)C)OC4=CC(OCCC)=CC(OCCCCN(C)C)=C4)=O.FC(F)(C(O)=O)F |
安全信息
| 储存分类代码 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
m.cnreagent.com
