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MEK1/2 Inhibitor IV-CAS 212631-67-9-Calbiochem
| 产品编号： | 4084104 |
| 规格： | The MEK1/2 Inhibitor IV, also referenced under CAS 212631-67-9, controls the biological activity of MEK1/2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. |
| CAS NO： | 212631-67-9 |
| 包装规格： | 5 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 |
| 4084104 | 5 MG | 3240 |
产品别名
212631-67-9
MEK1/2 Inhibitor IV-CAS 212631-67-9-Calbiochem
MEK Inhibitor IV, 2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluoro-5-bromo-benzamide, PD184161
2-(2-Chloro-4-iodo-phenylamino)-N-cyclopropylmethoxy-3,4-difluoro-5-bromo-benzamide, PD184161, MEK Inhibitor IV
基本信息
| Empirical Formula【经验(实验)分子式】 | C17H13BrClF2IN2O2 |
| Molecular weight | 557.56 |
| MDL number | MFCD16038897 |
| General description【一般描述】 | A cell-permeable, blood-brain barrier permeant, and orally active hydroxamate compound that is reported to inhibit MEK activity (IC50 = 10-100 nM) without competing against ATP or Erk binding and exhibit excellent selectivity over 27 other cellular kinases, including JNK, MAPK2/ERK2, SAPK2a, SAPK2b, SAPK3, and SAPK4 (IC50 >10 M). Shown to be superior to PD 98059 and U0126 in suppressing Erk1/2 phosphorylation in Hep3B, HepG2, PLC, and SKHep human liver cancer cells (IC50<0.1 M) in vitro and effectively reduce Erk1/2 phosphorylation in hippocampal tissue in mice (ED50<50 mg/kg, i.p.) in vivo. Both PD184161 and U0126 are shown to induce necrosis of several types of glucose-deprived cells via an indirect action on the F0 component of the mitochondrial F1F0-ATPase/synthase. A cell-permeable, blood-brain barrier permeant, and orally active hydroxamate compound that is reported to inhibit MEK activity (IC50 = 10-100 nM) without competing against ATP or Erk binding and exhibit excellent selectivity over 27 other cellular kinases, including JNK, MAPK2/ERK2, SAPK2a, SAPK2b, SAPK3, and SAPK4 (IC50 >10 µM). Shown to be superior to PD 98059 (Cat. Nos. 513000 and 513001 and U0126 (Cat. No. 662005) in suppressing Erk1/2 phosphorylation in Hep3B, HepG2, PLC, and SKHep human liver cancer cells (IC50<0.1 µM) in vitro and effectively reduce Erk1/2 phosphorylation in hippocampal tissue in mice (ED50<50 mg/kg, i.p.) in vivo. Both PD184161 and U0126 are shown to induce necrosis of several types of glucose-deprived cells via an indirect action on the F0 component of the mitochondrial F1F0-ATPase/synthase. |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. |
| Other Notes【其他说明】 | Yip-Schneider, M.T., et al. 2009. J. Pharmacol. Exp. Ther.329, 1063. Duman, C.H., et al. 2007. Biol. Psychiatry61, 661. Klein, P.J., et al. 2006. Neoplasia8, 1. Thottassery, J.V., et al. 2004. Cancer Res.64, 4637. Yung, H.W., et al. 2004. Biochem. Pharmacol.68, 351. |
| 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】 | ≥98% (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: 100 mg/mL ethanol: 5 mg/mL |
| shipped in【运输】 | ambient |
| storage temp.【储存温度】 | 2-8℃ |
| packaging【包装】 | Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
