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KPT-6566

Chemical Structure : KPT-6566

CAS No.: 881487-77-0

KPT-6566 (KPT 6566, KPT6566)

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.

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Biological Activity

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.

Physicochemical Properties

M.Wt 443.532
Formula C22H21NO5S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Acetic acid, 2-[[4-[[[4-(1,1-dimethylethyl)phenyl]sulfonyl]imino]-1,4-dihydro-1-oxo-2-naphthalenyl]thio]-

References

1. Campaner E, et al. Nat Commun. 2017 Jun 9;8:15772.

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