KYP 2047

Biological Activity

KYP 2047 is a high affinity prolyl oligopeptidase (POP) inhibitor (K_i = 0.023 nM). Clears α-synuclein aggregates induced by oxidative stress in neuronal cells. Inhibits the formation of AcSDKP from its precursor 43-mer thymosin β4 (Tβ4). Induces angiogenesis via POP inhibition. It reduces tau aggregation in tau-transfected HEK-293 cells and N2A cells as well as in human iPSC-derived neurons from patients with frontotemporal dementia. In vivo, treatment with KYP 2047 of transgenic mice with tauopathy, reduces tau aggregation in the brain and cerebrospinal fluid and slows cognitive decline. Anti-angiogenic and neuroprotective. Brain penetrant.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Binding kinetics and duration of in vivo action of novel prolyl oligopeptidase inhibitors.
   Venäläinen et al.
   Biochem.Pharmacol., 2006;71:683
2. A prolyl oligopeptidase inhibitor, KYP-2047, reduces alpha-synuclein protein levels and aggregates in cellular and animal models of Parkinson's disease.
   Myöhänen et al.
   Br.J.Pharmacol., 2012;166:1097
3. Brain pharmacokinetics of two prolyl oligopeptidase inhibitors, JTP-4819 and KYP-2047, in the rat.
   Jalkanen et al.
   Basic Clin.Pharmacol.Toxicol., 2011;109:443
4. Prolyl oligopeptidase induces angiogenesis both in vitro and in vivo in a novel regulatory manner.
   Myöhänen et al.
   Br.J.Pharmacol., 2011;163:1666
5. Inhibition of alpha-synuclein aggregation by multifunctional Da agonists assessed by a novel in vitro assay and an in vivo Drosophila synucleinopathy model.
   Yedlapudi et al.
   Sci Rep., 2016;69:38510

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