产品说明
一般描述
A reversible, cell-permeable pyrazolone p300/CBP HAT inhibitor (Ki = 400 nM), which competes with acetyl-CoA for the p300 Lys-CoA binding pocket. This compound demonstrates 86% inhibition against p300 at 10 nM, but elicits less than 10% inhibition against serotonin N-acetyltransferase, PCAF histone acetyltransferase, GCN5 histone acetyletransferase, Rtt109 histone acetyletransferase, Sas histone acetyl transferase, and MOZ histone acetyltransferase in a chemical screening assay. Treatment of C3H 10T1/2 mouse fibroblasts with 25 µM of compound results in an inhibitory effect against basal and TSA-inducible acetylation of histones H3 and H4. It is also shown to inhibit human cell growth in both melanoma and non-small-cell-lung (NSCL) cancer cell lines at 10 µM with similar or higher potency compared with that of the peptide-based bisubstrate p300/CBP HAT inhibitor Lys-CoA-Tat at 25 µM.
包装
10 mg in Plastic ampoule
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 3 months at -20°C.
其他说明
Bowers, EM., et al. 2010. Chem Biol17, 471.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C24H19N3O6 |
| 分子量 | 445.42 |
| MDL编号 | MFCD01784780 |
| NACRES | NA.77 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥99% (sum of isomers, HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze protect from light |
| 颜色 | brick red |
| 溶解性 | DMSO: 50 mg/mL |
| 运输 | ambient |
| 储存温度 | −20℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
