MilliporeSigma™ Calbiochem™ SKP2 E3 Ligase Inhibitor III

Description

A cell-permeable benzothiazolylchromenone compound that disrupts Skp2-Skp1 interaction via direct Skp2 affinity binding and selectively prevents Skp2-, but not Fbw7- or β-TrCP-, Skp1-Cullin-1-F-box (SFC) complex-mediated substrates ubiquitination, effectively preventing Skp2 substrates activation (Akt) and degradation (p21 & p27) with concomitant down-regulation of cellular Skp2 protein level (10 to 20μM in HEK293T & PC3 cultures)

A cell-permeable benzothiazolylchromenone compound that disrupts Skp2-Skp1 interaction via direct Skp2 affinity binding and selectively prevents Skp2-, but not Fbw7- or β-TrCP-, Skp1-Cullin-1-F-box (SFC) complex-mediated substrates ubiquitination, effectively preventing Skp2 substrates activation (Akt) and degradation (p21 & p27) with concomitant down-regulation of cellular Skp2 protein level (10 to 20μM in HEK293T & PC3 cultures). Exhibits antiproliferation activity toward a panel of 8 cancer (IC₅₀ from 1.22 to 10.5μM) and reduces ALDH⁺ cancer stem cell population in PC3 cultures (10 to 20μM). Exhibits good pharmacokinetic property and is efficacious in suppressing A549 and PC3 tumor growth in mice (40 to 80mg/kg/d i.p.) in vivo .

Specifications

• Color: Beige
• Description: 98% by HPLC
• Target Proteins: Skp2
• Molecular Formula: C₂₄H₂₄N₂O₃S
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Powder
• Quantity: 10 mg