85-2076-85　［取扱停止］SKP2 E3 Ligase Inhibitor III (p27/Kip1 Activator III, S-phase Kinase-associated Protein 2 Inhibitor III, SCFSKP2 Inhibitor III, SZL-P1-41, 3-(1,3-Benzothiazol-2-yl)-6-ethyl-7-hydroxy-8-(1-piperidinylmethyl)-4H-chromen-4-one, 3-(Benzo[d]thiazol-2-yl)-6-ethyl-7-hydroxy-8-(piperidin-1-ylmethyl)-4H-chromen-4-one, 3-Benzothiazol-2-yl-6-ethyl-7-hydroxy-8-(piperidylmethyl)chromen-4-one, ...　217796

特徴

• A cell-permeable benzothiazolylchromenone compound that disrupts Skp2-Skp1 interaction via direct Skp2 affinity binding and selectively prevents Skp2-, but not Fbw7- or beta-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 20uM in HEK293T & PC3 cultures). Exhibits antiproliferation activity toward a panel of 8 cancer (IC50 from 1.22 to 10.5uM) and reduces ALDH+ cancer stem cell population in PC3 cultures (10 to 20uM). 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.
• Synonyms:3-(1,3-Benzothiazol-2-yl)-6-ethyl-7-hydroxy-8-(1-piperidinylmethyl)-4H-chromen-4-one, 3-(Benzo[d]thiazol-2-yl)-6-ethyl-7-hydroxy-8-(piperidin-1-ylmethyl)-4H-chromen-4-one, 3-Benzothiazol-2-yl-6-ethyl-7-hydroxy-8-(piperidylmethyl)chromen-4-one, p21/Cip1/CKI/Waf1 Activator III, CRL1SKP2 Inhibitor III, p27/Kip1 Activator III, S-phase Kinase-associated Protein 2 Inhibitor III, SCFSKP2 Inhibitor III, SZL-P1-41
• Molecular Formula:C₂₄H₂₄N₂O₃S
• Solubility:DMSO
• Primary Target:Skp2
• Purity:≥98% (HPLC)
• Form:Supplied as a beige powder.
• Storage and Stability:May be stored at 4°C for short-term only. Long-term storage is recommended at -20°C. Stable for 1 year after receipt. Protect from light. For maximum recovery of product, centrifuge the original vial prior to removing the cap.