KPT-6566

KPT-6566

CAT N°: 37308
Price:

From 128.00 108.80

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.{67145} 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.

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