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KPT-6566 

Cat. No. M30801
KPT-6566  Structure
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Biological Activity

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.

Chemical Information
Molecular Weight 443.54
Formula C22H21NO5S2
CAS Number 881487-77-0
Form Solid
Solubility (25°C) DMSO 19.23 mg/mL (ultrasonic)
Storage 4°C, protect from light, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Zheng Zhang, et al. Acta Biochim Biophys Sin (Shanghai). Inhibition of the PIN1-NRF2/GPX4 axis imparts sensitivity to cisplatin in cervical cancer cells

[2] Yan-Tong Guo, et al. Aging Dis. Predictive Value of Pin1 in Cervical Low-Grade Squamous Intraepithelial Lesions and Inhibition of Pin1 Exerts Potent Anticancer Activity against Human Cervical Cancer

[3] Elena Campaner, et al. Nat Commun. A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action

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  Catalog
Abmole Inhibitor Catalog




Keywords: KPT-6566  supplier, inhibitors, activators


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