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SKP2 E3 Ligase Inhibitor I, C1-CAS 432001-69-9-Calbiochem
产品别名
432001-69-9
SKP2 E3 Ligase Inhibitor I, C1-CAS 432001-69-9-Calbiochem
p21/Cip1/Waf1 Activator I; p27/Kip1 Activator I, S-phase Kinase-associated Protein 2 Inhibitor I; SCF SKP2 Inhibitor I, CRL1 SKP2 Inhibitor I, ( Z)-2-(4-Bromo-2-((4-oxo-3-(pyridin-3-ylmethyl)-2-thioxothiazolidin-5-ylidene)met
基本信息
Empirical Formula【经验(实验)分子式】 | C18H13BrN2O4S2 |
Molecular weight | 465.34 |
General description【一般描述】 | A cell-permeable rhodanine compound that upregulates cellular p21Cip1/Waf1 and p27Kip1 protein levels (10 µM for 16 h in 501 Mel cultures) by preventing Skp2-Cks1-mediated substrate recruitment without affecting the F-box E3 ubiquitin ligase Skp2 interaction with Cks1 or the SCF (Skp1-cullin1-F-box) complex. Shown to inhibit the proliferation of human breast cancer MCF-7 and melanoma 501 Mel cells (IC50 = 8 and 30 µM, respectively; 16 h incubation). Unlike SMIP004 (Cat. No. 500517), C1 does not affect cellular Cyclin E/CDK2 kinase activity or Skp2 level. Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water. A cell-permeable rhodanine compound that upregulates cellular p21Cip1/Waf1 and p27Kip1 protein levels (10 µM for 16 h in 501 Mel cultures) by preventing Skp2-Cks1 (Cdc kinase subunit 1)-mediated substrate recruitment without affecting the F-box E3 ubiquitin ligase Skp2 interaction with Cks1 or the SCF (Skp1-cullin1-F-box) complex. Shown to inhibit the proliferation of human breast cancer MCF-7 and melanoma 501 Mel cells (IC50 = 8 and 30 µM; 16 h incubation). Unlike SMIP004 (Cat. No. 567314), C1 does not affect cellular Cyclin E/CDK2 kinase activity or Skp2 level. |
Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Primary Target disrupts p27-Skp2 interaction Reversible: yes |
Warning【警告】 | Toxicity: Standard Handling (A) |
Reconstitution【重悬】 | Use only fresh DMSO for reconstitution. 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】 | Rico-Bautista, E., and Wolf, D.A. 2012. Chem. Biol.19, 1497. Wu, L., et al. 2012. Chem. Biol.19, 1515. |
Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
Assay【测定】 | ≥99% (HPLC) |
Quality Level【质量水平】 | 100 |
form【形式】 | powder |
manufacturer/tradename | Calbiochem® |
storage condition【储存条件】 | OK to freeze protect from light |
color【颜色】 | orange-brown |
solubility【溶解性】 | DMSO: 10 mg/mL |
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 2 |