Prokineticin 2 Antagonist, PKRA7

A cell permeable, brain permeant 3-pyrrolidine carboxamide derivative that acts as an antagonist of polypeptide chemokine prokineticin 2 (PK2) receptor (Bv8, PROK2; IC₅₀ = 5 nM and 8.2 nM for PKR1 and PKR2, respectively). Suppresses the growth of D456MG glioma cell xenografts in nude mice by reducing blood vessel density and blocking angiogenesis via inhibition of PKR1 and PKR2 expressed on endothelial cells. Shown to suppress the growth of AsPC1 and CFPac-1 pancreatic tumor cells in xenograft model of nude mice by reducing macrophage migration and inflitration. Reduces the expression of CCL27, CCR10, CCR4, CCR5, and CCR6 pro-migratory chemokines and chemokine receptors in macrophages. Enhances the efficacy of standard temomolomide in the treatment of glioblastoma and gemcitabine in the treatment of pancreatic cancer in xenograft nude mice models.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Primary Target
PROK2

Reversible: yes

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Curtis, V., et al. 2013. PLoS One.8, e54916.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)