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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 Size | Price | Availability | Quantity |
---|---|---|---|
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 |
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. |
Molecular Weight | 443.54 |
Formula | C22H21NO5S2 |
Cas No. | 881487-77-0 |
Smiles | CC(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 | Powder: -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
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