KYP 2047
Modify Date: 2024-01-07 18:43:37
KYP 2047 structure
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Common Name | KYP 2047 | ||
|---|---|---|---|---|
| CAS Number | 796874-99-2 | Molecular Weight | 339.43 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C20H25N3O2 | Melting Point | N/A | |
| MSDS | USA | Flash Point | N/A | |
| Symbol |
GHS07 |
Signal Word | Warning | |
Use of KYP 2047KYP-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]. |
| Name | KYP-2047 |
|---|
| Description | 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]. |
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| Related Catalog | |
| In Vitro | 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]. Cell Proliferation Assay Cell Line: U-87, U-138 and A-172 cell[2] Concentration: 0.01 μM, 0.1 μM, 0.5 μM, 1 μM, 10 μM, 30 μM, 50 μM and 100 μM Incubation Time: 24 h Result: Decreased U-87, U-138 and A-172 cell viability in a concentration-dependent manner. Western Blot Analysis Cell Line: U-87 cell[2] Concentration: 0, 50, 100 μM Incubation Time: 24 h Result: Increased the pro-apoptotic protein Bax, p53 and cleaved-caspase-3 expression, reduced significantly Bcl2 expression, reduced Ang1 and Ang2 expression, and decreased Ki-67 expression. |
| In Vivo | 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]. |
| References |
| Molecular Formula | C20H25N3O2 |
|---|---|
| Molecular Weight | 339.43 |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H319 |
| Precautionary Statements | P305 + P351 + P338 |
| RIDADR | NONH for all modes of transport |
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A prolyl oligopeptidase inhibitor, KYP-2047, reduces α-synuclein protein levels and aggregates in cellular and animal models of Parkinson's disease.
Br. J. Pharmacol. 166(3) , 1097-113, (2012) The aggregation of α-synuclein is connected to the pathology of Parkinson's disease and prolyl oligopeptidase (PREP) accelerates the aggregation of α-synuclein in vitro. The aim of this study was to i... |