半岛bd体育手机客户端 说明
一般描述
A cell-permeable hydroxyphenyl-propylidene-benzohydrazide compound that acts as a potent, ATP-competitive (Ki= 0.3 ?M), and highly isoform-selective PIM inhibitor (IC50= 2.5, 2.5, and 0.047 ?M against PIM1, PIM2, and PIM3, respectively; [ATP] = 10 ?M), while affecting CK2α2 only at much higher concentrations (IC50= 5 ?M, [ATP] = 10 ?M) and exhibiting little or no activity against a panel of 258 other kinases (<40% inhibition at 5 ?M). Shown to inhibit PIM3-dependent STAT3 Tyr705 phosphorylation in DU-145 prostate cancer and MiaPaCa2 pancreatic cancer cells (by 73% and 83%, respectively; 10 ?M for 18 h), while displaying little effect toward STAT3 Tyr694 phosphoylation in 22RV1 cultures.
A cell-permeable hydroxyphenyl-propylidene-benzohydrazide compound that acts as a potent, ATP-competitive (Ki= 0.3 ?M), and highly isoform-selective PIM inhibitor (IC50= 2.5, 2.5, and 0.047 ?M against PIM1, PIM2, and PIM3, respectively, with PIMtide as substrate, [ATP] = 10 ?M), while affecting CK2α2 only at much higher concentrations (IC50= 5 ?M, [ATP] = 10 ?M) and exhibiting little or no activity against a panel of 258 other kinases (<40% inhibition; [M-110] = 5 ?M). M-100 treatment (10 ?M for 18 hr) is shown to inhibit both basal (by 73% and 83% of DMSO control in DU-145 prostate cancer and MiaPaCa2 pancreatic cancer cells, respectively) and IL-6-stimulated (by 69% of DMSO control in DU-145 cells) STAT3 phosphorylation on Tyr705, while displaying little effect toward Tyr694 phosphoylation (in 22RV1 cultures). Isoform-specific knockdowns in DU-145 cells likewise identify PIM-3, but not PIM-1 or -2, as the kinase responsible for cellular STAT3 Tyr705 phosphorylation.
包装
10 mg in Glass bottle
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 6 months at -20°C.
其他说明
Chang, M., et al. 2010.Mol. Cancer Ther.9,2478.
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 | C22H28ClN5O3 |
| 分子量 | 445.94 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥97% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze protect from light |
| 颜色 | pale yellow |
| 溶解性 | DMSO: 50 mg/mL |
| 运输 | wet ice |
| 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 |
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