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KPT-6566

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Catalog No. T5994Cas No. 881487-77-0

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.

KPT-6566

KPT-6566

🥰Excellent
Purity: 97.81%
Catalog No. T5994Cas No. 881487-77-0
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.
Pack SizePriceAvailabilityQuantity
1 mg$97 In Stock
2 mg$148 In Stock
5 mg$297 In Stock
10 mg$455 In Stock
25 mg$753 In Stock
50 mg$1,060 In Stock
100 mg$1,430 In Stock
1 mL x 10 mM (in DMSO)$289 In Stock
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Purity:97.81%
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Product Introduction

Bioactivity
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.
Targets&IC50
PIN1 PPIase:640 nM
In vitro
KPT-6566 covalently binds to the catalytic site of PIN1,inhibited the PPIase activity of PIN1 and turned out to have an IC50 of 0.64 μM.?This interaction results in the release of a quinone-mimicking drug that generates reactive oxygen species and DNA damage, inducing cell death specifically in cancer cells.
Cell Research
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.
Chemical Properties
Molecular Weight443.54
FormulaC22H21NO5S2
Cas No.881487-77-0
SmilesCC(C)(C)c1ccc(cc1)S(=O)(=O)\N=C1/C=C(SCC(O)=O)C(=O)c2ccccc12
Relative Density.1.32 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 120 mg/mL (270.55 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2546 mL11.2729 mL22.5459 mL112.7294 mL
5 mM0.4509 mL2.2546 mL4.5092 mL22.5459 mL
10 mM0.2255 mL1.1273 mL2.2546 mL11.2729 mL
20 mM0.1127 mL0.5636 mL1.1273 mL5.6365 mL
50 mM0.0451 mL0.2255 mL0.4509 mL2.2546 mL
100 mM0.0225 mL0.1127 mL0.2255 mL1.1273 mL

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