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Chk2 Inhibitor, PV1019-Calbiochem
| 产品编号： | 4155666 |
| 规格： | The Chk2 Inhibitor, PV1019 controls the biological activity of Chk2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. |
| 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 |
产品别名
Chk2 Inhibitor, PV1019-Calbiochem
NSC 744039
基本信息
| Empirical Formula【经验(实验)分子式】 | C18H17N7O3 |
| Molecular weight | 379.37 |
| General description【一般描述】 | A cell-permeable nitroindolo-guanidinohydrazone compound that acts as a potent, ATP-competitive, and highly selective Chk2 inhibitor (IC50 = 138 and 570 nM against the phosphorylation of histone H1 by Chk2 in the presence of 10 µM and 1 mM of ATP, respectively), while exhibiting much reduced or no activity against a panel of 52 other cellular kinases, including Chk1 (IC50 = 15.73 and 55 µM against substrate phosphorylation and Chk1 autophosphorylation with 10 µM ATP). Shown to effectively suppress radiation-induced phosphorylation of Chk2 (on Ser516) and its downstream substrate Cdc25c (on Ser216) in MCF7 cultures (IC50<10 µM) and reduce the sensitivity of wild-type murine thymocytes to radiation-induced apoptosis to the level seen in Chk2-/- cultures. A cell-permeable nitroindolo-guanidinohydrazone compound that acts as a potent, ATP-competitive, and highly selective Chk2 inhibitor (IC50 = 138 and 570 nM against the phosphorylation of histone H1 by Chk2 in the presence of 10 µM and 1 mM of ATP, respectively), while exhibiting much reduced or no activity against a panel of 52 other cellular kinases, including Chk1 (IC50 = 15.73 and 55 µM against substrate phosphorylation and Chk1 autophosphorylation with 10 µM ATP). Shown to effectively suppress radiation-induced phosphorylation of Chk2 (on Ser516) and its downstream substrate Cdc25c (on Ser216) in MCF7 cultures (IC50<10 µM) and reduce the sensitivity of wild-type murine thymocytes to radiation-induced apoptosis to the level seen in Chk2-/- cultures. |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Reconstitution【重悬】 | Following reconstitution, aliqout and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. |
| Other Notes【其他说明】 | Jobson, A.G., et al. 2009. J. Pharmacol. Exp. Ther.331, 816. |
| 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】 | ≥95% (HPLC) |
| form【形式】 | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze desiccated (hygroscopic) protect from light |
| color【颜色】 | orange |
| solubility【溶解性】 | DMSO: 5 mg/mL |
| shipped in【运输】 | ambient |
| storage temp.【储存温度】 | −20℃ |
| 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 |
