A covalent PIN1 inhibitor
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KPT-6566

Item No. 37308

Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[4-[[[4-(1,1-dimethylethyl)phenyl]sulfonyl]imino]-1,4-dihydro-1-oxo-2-naphthalenyl]thio]-acetic acid
CAS Number
881487-77-0
Molecular Formula
C22H21NO5S2
Formula Weight
443.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
224, 260, 324 nm
SMILES
O=C(CSC1=CC(C2=C(C1=O)C=CC=C2)=NS(=O)(C3=CC=C(C(C)(C)C)C=C3)=O)O
InChi Code
InChI=1S/C22H21NO5S2/c1-22(2,3)14-8-10-15(11-9-14)30(27,28)23-18-12-19(29-13-20(24)25)21(26)17-7-5-4-6-16(17)18/h4-12H,13H2,1-3H3,(H,24,25)
InChi Key
BXWWOKYIKNEEHJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $94

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    10 mg

    $179

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    25 mg

    $418

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    50 mg

    $789

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    Cayman Chemical
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    Product Description

    KPT-6566 is a covalent inhibitor of peptidylprolyl cis/trans isomerase, NIMA-interacting 1 (PIN1; IC50 = 0.64 µM), an enzyme that catalyzes cis-trans or trans-cis conformational changes around serine-phosphate or threonine-phosphate bonds.1 It inhibits cell proliferation, decreases hyperphosphorylation of phosphorylated retinoblastoma protein (pRb), and reduces cyclin D1 levels in wild-type, but not Pin1-/-, mouse embryonic fibroblasts (MEFs). KPT-6566 inhibits colony formation (IC50 = 1.2 µM) and impairs secondary mammosphere formation, a marker of cancer stem cell activity, by MDA-MB-231 cells. In vivo, KPT-6566 (5 mg/kg) reduces the number of lung metastases in an MDA-MB-231 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Campaner, E., Rustighi, A., Zannini, A., et al. A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action. Nat. Commun. 8(1), 15772 (2017).