半岛bd体育手机客户端 说明
一般描述
A cell-permeable pyrazolylthiazolo-isobutyramide compound that acts as a potent LIM kinase inhibitor (IC50= 7 and 8 nM against LIMK1 and LIMK2, respectively) and effectively suppresses cellular cofilin phosphorylation (IC50~ 1 ?M in A549 and MDA-MB-231 cultures) without affecting tubulin polymerization or inducing cytotoxicity (EC50>10 ?M in A549 proliferation and colony formation assays). Shown to effectively destabilize F-actin structure in MDA-MB-231 breast cancer cells (3 to 10 ?M) with concomitant blockage of invadopedia-mediated ECM degradation (13% and 10% of control, respectively, by 3 and 10 ?M inhibitor) and invasion (45% and 7% of control invasion rate, respectively, by 3 and 10 ?M inhibitor). Although reported to exhibit affinity toward AMPKα1 and AMPKα2 in T7 phage-based competition binding studies, inhibitory activity of LIMKi 3 against AMPKα1/2 is not yet directly demonstrated.
A cell-permeable pyrazolylthiazolo-isobutyramide compound that acts as a potent LIM kinase inhibitor (IC50= 7 and 8 nM against LIMK1 and LIMK2, respectively) and effectively suppresses cellular cofilin phosphorylation (IC50 ~ 1 ?M in A549 and MDA-MB-231 cultures) without affecting tubulin polymerization or inducing cytotoxicity (EC50>10 ?M in A549 proliferation & colony formation assays). Shown to effectively destabilize F-actin structure in MDA-MB-231 breast cancer cells (3 to 10 ?M) with concomitant blockage of invasion (by 93% at 10 ?M).
包装
10 mg in Glass bottle
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Target IC50: 7 and 8 nM against LIMK1 and LIMK2, respectively
Primary Target
LIMK1 and LIMK2
Reversible: yes
Secondary Target
AMPKA1, AMPKA2, DDR1, PAK3, DCAMKL2
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
Scott, R.W., et al. 2010.J. Cell. Biol.191,169.
Ross-Macdonald, P., et al. 2008.Mol. Cancer Ther.7,3490.
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 | C17H14Cl2F2N4OS |
| 分子量 | 431.29 |
| MDL编号 | MFCD17019327 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥95% (HPLC) |
| 形式 | powder |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze protect from light |
| 颜色 | beige |
| 溶解性 | DMSO: 100 mg/mL |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
| SMILES string | ClC1=CC=CC(Cl)=C1N2N=C(C=C2C3=CN=C(NC(C(C)C)=O)S3)C(F)F |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 2 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
