您的位置:首页 > 产品中心 > 285983-48-4, p38 MAP Kinase Inhibitor X, BIRB 796-CAS 285983-48-4-Calbiochem
p38 MAP Kinase Inhibitor X, BIRB 796-CAS 285983-48-4-Calbiochem
产品编号: | 4168277 |
规格: | The p38 MAP Kinase Inhibitor X, BIRB 796, also referenced under CAS 285983-48-4, controls the biological activity of p38 MAP Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. |
CAS NO: | 285983-48-4 |
包装规格: | 10 MG |
产品类别: | 进口试剂 |
品牌: | Sigma-Aldrich |
优惠价: | 立即咨询 |
产品价格查看更多规格...
产品编号 | 包装单位 | 单价(元) | 国内现货 | 国外库存 | 询价单 |
4168277 | 10 MG | 2380 |
产品别名
285983-48-4
p38 MAP Kinase Inhibitor X, BIRB 796-CAS 285983-48-4-Calbiochem
Doramapimod, BIRB796, 1-(5- tert-Butyl-2- p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, JNK Inhibitor XVII
Doramapimod, BIRB796, 1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea, JNK Inhibitor XVII
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C31H37N5O3 |
Molecular weight | 527.66 |
MDL number | MFCD09752957 |
General description【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). |
Warning【警告】 | Toxicity: Regulatory Review (Z) |
Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. |
Other Notes【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. |
Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥99% (HPLC) |
form【形式】 | solid |
manufacturer/tradename | Calbiochem® |
storage condition【储存条件】 | OK to freeze protect from light |
color【颜色】 | white |
solubility【溶解性】 | DMSO: 50 mg/mL, clear, colorless |
shipped in【运输】 | ambient |
storage temp.【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 |
packaging【包装】 | 10 mg in Glass bottle Packaged under inert gas |
安全信息
Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
WGK | WGK 3 |