PKRA83

Names

[ Name ]:
PKRA83

Biological Activity

[Description]:

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 and anti-angiogenic activities. PKRA83 can penetrate the blood-brain barrier[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Others >> Others

[Target]

IC50: 5.0 nM (PKR1) and 8.2 nM (PKR2)[1]

[In Vitro]

PKRA83 (PKRA7; 1 µg/mL) effectively reduces PK2-induced microvascular endothelial cell branching in vitro[1].

[In Vivo]

PKRA83 (PKRA7; 20 mg/kg; i.p) shows anti-tumor activity in the context of glioblastoma and pancreatic cancer xenograft tumor models. For the highly vascularized glioblastoma, PKRA83 (PKRA7) is associated with decreased blood vessel density and increased necrotic areas in the tumor mass[1].

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₇H₃₄ClFN₂O₄

[ Molecular Weight ]:
505.02

Related Compounds

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