KYP-2047

• CAT Number: I007545
• CAS Number: 796874-99-2
• Molecular Formula: C20H25N3O2
• Molecular Weight: 339.43
• Purity: ≥95%
• Synonyms: (2S)-1-[(2S)-1-(4-phenylbutanoyl)pyrrolidine-2-carbonyl]pyrrolidine-2-carbonitrile
• InChI: InChI=1S/C20H25N3O2/c21-15-17-10-5-13-22(17)20(25)18-11-6-14-23(18)19(24)12-4-9-16-7-2-1-3-8-16/h1-3,7-8,17-18H,4-6,9-14H2/t17-,18-/m0/s1
• InChIKey: SPXFAUXQZWJGCJ-ROUUACIJSA-N
• SMILES: C1CC(N(C1)C(=O)C2CCCN2C(=O)CCCC3=CC=CC=C3)C#N

KYP-2047 is a potent and BBB-penetrating prolyl-oligopeptidase (POP) inhibitor, with an Ki value of 0.023 nM. KYP-2047 reduces glioblastoma proliferation through angiogenesis and apoptosis modulation[1][2].
KYP-2047 (0-100 μM) decreases U-87, U-138 and A-172 cell viability in a concentration-dependent manner[2].
KYP-2047 (0-100 μM) increases the pro-apoptotic protein Bax, p53 and caspase-3 expression whereas reduces Bcl-2 expression, and reduced significantly TGF-β expression[2].
KYP-2047 (1 or 5 mg/kg, 30 min before daily testing) dose-dependently improved the escape performance (i.e. latency to find the hidden platform and swimming path length) of the young but not the old rats in the water maze[1].
KYP-2047 (9 or 27 μmol/kg; IP; once, 1 or 3 h before decapitation; two daily doses for 10 days) increases neurotensin concentration in the hypothalamus[1].
KYP-2047 (0-5 mg/kg) significantly reduces tumor mass and neutrophil infiltration[2].
KYP-2047 (0-5 mg/kg) significantly reduces vascular endothelial-growth-factor (VEGF), CD34, angiopoietins (Ang) and endothelial-nitric-oxide synthase (eNOS) expression[2].

Reference

[1]. Jalkanen AJ, et al. Beneficial effect of prolyl oligopeptidase inhibition on spatial memory in young but not in old scopolamine-treated rats. Basic Clin Pharmacol Toxicol. 2007 Feb;100(2):132-8.
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[2]. Scuderi SA, et al. KYP-2047, an Inhibitor of Prolyl-Oligopeptidase, Reduces GlioBlastoma Proliferation through Angiogenesis and Apoptosis Modulation. Cancers (Basel). 2021 Jul 9;13(14):3444.
 [Content Brief]