PKRA83

PKRA83 (PKRA7) is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2 to its receptors PKR1 and PKR2. PKRA83 potently inhibits PK2 receptors, with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 has anticancer, anti-arthritis and anti-angiogenic activities. PKRA83 can penetrate the blood-brain barrier.

PKRA83 (1 µg/mL) effectively reduces PK2-induced microvascular endothelial cell branching in vitro^[1].
PKRA83 (2 μM, 24 h) blocks the neuroprotective action of rPK2 in dopaminergic N27 cells (rPK2 protects N27 cell against MPP⁺-induced dopaminergic neuronal cell death)^[3].

PKRA83 (20 mg/kg; i.p) shows anti-tumor activity in the context of glioblastoma xenograft tumor models^[1].
PKRA83 (15 mg/kg; i.p, daily for 2 weeks) inhibits arthritis in mice with collagen-induced arthritis^[2].

References:
[1]. Valerie F Curtis, et al. A PK2/Bv8/PROK2 antagonist suppresses tumorigenic processes by inhibiting angiogenesis in glioma and blocking myeloid cell infiltration in pancreatic cancer. PLoS One. 2013;8(1):e54916.
[2]. Ito H, et al. Prokineticin 2 antagonist, PKRA7 suppresses arthritis in mice with collagen-induced arthritis. BMC Musculoskelet Disord. 2016 Sep 8;17(1):387.
[3]. Gordon R, et al. Prokineticin-2 upregulation during neuronal injury mediates a compensatory protective response against dopaminergic neuronal degeneration. Nat Commun. 2016 Oct 5;7:12932.