产品说明
一般描述
A cell-permeable pyrazolo-napthalenyl urea compound that acts as a highly potent, slowly binding (IC50 = 8 and 97 nM, respectively, against human p38α, respectively, with or without 2 h preincubation), but high affinity (t1/2 of dissociation from human p38α = 23 h), p38-selective inhibitor by simultaneously targeting the ATP-binding site and an adjacent DFG-out conformation-specific allosteric cavity. It inhibits JNK2α2 and c-Raf-1 only at much higher concentrations (IC50 = 98 nM and 1.4 µM, respectively) and displays little or no activity toward 10 other kinases (IC50 >20 µM). Shown to inhibit LPS-induced TNF-α production both in vitro (IC50 = 18 and 780 nM using THP-1 cells and in human whole blood, respectively) and in mice in vivo (by 84%; 30 mg/kg p.o.).
A cell-permeable pyrazolo-napthalenyl urea compound that acts as a highly potent, slowly binding (IC50 = 8 and 97 nM, respectively, against human p38α, respectively, with or without 2 h preincubation), but high affinity (t1/2 of dissociation from human p38α = 23 h), p38-selective inhibitor by simultaneously targeting the ATP-binding site and an adjacent DFG-out conformation-specific allosteric cavity. It inhibits JNK2α2 and c-Raf-1 only at much higher concentrations (IC50 = 98 nM and 1.4 µM, respectively) and displays little or no activity toward 10 other kinases (IC50 >20 µM). Shown to inhibit LPS-induced TNF-α production in cultures in vitro (IC50 = 18 and 780 nM using THP-1 cells and in human whole blood, respectively) and in mice in vivo (by 84% and 63%, respectively, with oral dosage of 30 mg/kg and 10 mg/kg).
包装
10 mg in Glass bottle
Packaged under inert gas
警告
Toxicity: Regulatory Review (Z)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Liu. Y. and Gray, N.S., 2006. Nat. Chem. Biol.2, 358.
Regan, J., et al. 2003. J. Med. Chem.46, 4676.
Pargellis, C., et al. 2002. Nat. Struct. Biol.9, 268.
Regan, J., et al. 2002. J. Med. Chem.45, 2994.
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 | C31H37N5O3 |
| 分子量 | 527.66 |
| MDL编号 | MFCD09752957 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥99% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze protect from light |
| 颜色 | white |
| 溶解性 | DMSO: 50 mg/mL, clear, colorless |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
| SMILES string | CC1=CC=C(N2C(NC(NC3=CC=C(OCCN4CCOCC4)C5=C3C=CC=C5)=O)=CC(C(C)(C)C)=N2)C=C1 |
| InChI | 1S/C31H37N5O3/c1-22-9-11-23(12-10-22)36-29(21-28(34-36)31(2,3)4)33-30(37)32-26-13-14-27(25-8-6-5-7-24(25)26)39-20-17-35-15-18-38-19-16-35/h5-14,21H,15-20H2,1-4H3,(H2,32,33,37) |
| InChI key | MVCOAUNKQVWQHZ-UHFFFAOYSA-N |
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 |
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