Formulation: A solid
Formal Name: 2-[[4-[[[4-(1,1-dimethylethyl)phenyl]sulfonyl]imino]-1,4-dihydro-1-oxo-2-naphthalenyl]thio]-acetic acid
Purity: ≥98%
Formula Markup: C22H21NO5S2
Formula Weight: 443,5
Shelf life (days): 1460
CAS Number: 881487-77-0
Notes: 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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