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Bioactivity KPT-6566 is a selective and covalent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 value of 640 nM and a Ki value of 625.2 nM for PIN1 PPIase domain. KPT-6566 can be used for the research of cancer[1].
Target IC50: 640 nM (PIN1 PPIase)Ki: 625.2 nM (PIN1 PPIase)
Invitro KPT-6566 (1-5 μM; 0-8 d) inhibits WT fibroblasts proliferation[1].KPT-6566 (0-10 μM; 48 h) inhibits normal breast epithelial cells and cancer cells viability via a PIN1-dependent manner[1].KPT-6566 (0-10 μM; 48 h) affects hyperphosphorylated pRB level, Cyclin D1 and PIN1 concentration[1].KPT-6566 (2.5-5 μM; 48 h) inhibits the mut-p53, NOTCH1 and NRF2 pathways[1].KPT-6566 (0-5 μM; 48 h) induces DNA damage via a PIN1-dependent way[1]. Cell Proliferation Assay[1] Cell Line:
In Vivo KPT-6566 (5 mg/kg; i.p. once a day for 26 days) shows no toxicity to mice[1]. Animal Model:
Name KPT-6566
CAS 881487-77-0
Formula C22H21NO5S2
Molar Mass 443.54
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Reference [1]. Campaner E, et al. A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action. Nat Commun. 2017 Jun 9;8:15772.

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