MilliporeSigma™ Calbiochem™ SKP2 E3 Ligase Inhibitor I, C1

Description

A cell-permeable rhodanine compound that upregulates cellular p21^Cip1/Waf1 and p27^Kip1 protein levels (10μM 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) c

A cell-permeable rhodanine compound that upregulates cellular p21^Cip1/Waf1 and p27^Kip1 protein levels (10μM 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 30μM, 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.

Specifications

• Color: Orange Brown
• Description: 99% by HPLC
• Target Proteins: disrupts p27-Skp2 interaction
• Molecular Formula: C₁₈H₁₃BrN₂O₄S₂
• Formula Weight: 465.3g/mol
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Powder
• Quantity: 25 mg