| Description | KPT-6566 is a novel selective covalent pin1 inhibitor, KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain,and has anti-cancer activity. |
| In vitro | KPT-6566与PIN1的催化位点形成共价结合，抑制了PIN1的PPIase活性，并显示出0.64μM的IC50值。这种相互作用导致释放类醌药物，产生活性氧物种和DNA损伤，特异性地诱导癌细胞死亡。 |
| Cell experiments | For IC50 determination, human recombinant PIN1 was preincubated with different concentrations of KPT-6566 and PPIase activity was measured after 180 min. K values of PPIase activity were plotted against inhibitor concentration in a semi-logarithmic plot. |
| Target activity | PIN1 PPIase:640 nM |
| Synonyms | 2-[[4-[[[4-(叔丁基)苯基]磺酰基]亚氨基]-1-氧代-1,4-二氢-2-萘基]硫基]乙酸 |
| molecular weight | 443.54 |
| Molecular formula | C22H21NO5S2 |
| CAS | 881487-77-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 120 mg/mL (270.55 mM) |
| References | 1. Zhang J , Zhao F , Yu X , et al. Pharmacokinetics of eupalinolide A, eupalinolide B and hyperoside from Eupatorium lindleyanum in rats by LC/MS/MS[J]. Journal of Chromatography B, 2015, 995-996:1-7. |