KPT-6566

• CAT Number: I018140
• CAS Number: 881487-77-0
• Molecular Formula: C22H21NO5S2
• Molecular Weight: 443.54
• Purity: ≥95%
• Synonyms: 2-[(4E)-4-(4-tert-butylphenyl)sulfonylimino-1-oxonaphthalen-2-yl]sulfanylacetic acid
• InChI: 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)/b23-18+
• InChIKey: BXWWOKYIKNEEHJ-PTGBLXJZSA-N
• SMILES: CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)N=C2C=C(C(=O)C3=CC=CC=C32)SCC(=O)O

KPT-6566 is a selective and covalent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 value of 640 nM and a Ki value of 625.2 nM for PIN1 PPIase domain. KPT-6566 can be used for the research of cancer[1].
KPT-6566 (1-5 μM; 0-8 d) inhibits WT fibroblasts proliferation[1].
KPT-6566 (0-10 μM; 48 h) inhibits normal breast epithelial cells and cancer cells viability via a PIN1-dependent manner[1].
KPT-6566 (0-10 μM; 48 h) affects hyperphosphorylated pRB level, Cyclin D1 and PIN1 concentration[1].
KPT-6566 (2.5-5 μM; 48 h) inhibits the mut-p53, NOTCH1 and NRF2 pathways[1].
KPT-6566 (0-5 μM; 48 h) induces DNA damage via a PIN1-dependent way[1].
KPT-6566 (5 mg/kg; i.p. once a day for 26 days) shows no toxicity to mice[1].

Reference

[1]. Campaner E, et al. A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action. Nat Commun. 2017 Jun 9;8:15772.
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