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Chemical Structure : KPT-6566
CAS No.: 881487-77-0
Catalog No.: PC-61182Not For Human Use, Lab Use Only.
KPT-6566 (KPT6566) is a potent, specific and covalent inhibitor of the prolyl isomerase PIN1 with Ki of 625.2 nM, IC50 of 0.64 uM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $198 | In stock | |
| 25 mg | $298 | In stock | |
| 50 mg | $428 | In stock | |
| 100 mg | $728 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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KPT-6566 (KPT6566) is a potent, specific and covalent inhibitor of the prolyl isomerase PIN1 with Ki of 625.2 nM, IC50 of 0.64 uM.
KPT-6566 dispplays no activity against other PPIases, including GFKBP4 and PPIA.
KPT-6566 covalently binds to the catalytic site of PIN1, decreases the expression levels of mut-p53 and NOTCH1 target genes, inhibits colony forming efficiency in MDA-MB-231 cells (IC50=1.2 uM) through specific PIN1 inhibition.
KPT-6566 curbs self-renewal of breast cancer stem cells and promotes degradation of PIN1, elicits cellular responses to oxidative stress and induces DNA damage in a PIN1-dependent manner, induces cell death of cancer cells and reduces metastasis growth in vivo.
| M.Wt | 443.532 | |
| Formula | C22H21NO5S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Acetic acid, 2-[[4-[[[4-(1,1-dimethylethyl)phenyl]sulfonyl]imino]-1,4-dihydro-1-oxo-2-naphthalenyl]thio]- |
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1. Campaner E, et al. Nat Commun. 2017 Jun 9;8:15772.
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