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[1][2][3].

Product Specifications

CAS Number

[1233926-87-8]

Product Name Alternative

PKRA7

UNSPSC

12352005

Target

Prokineticin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Cancer-programmed cell death

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/pkra83.html

Purity

98.95

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

ClC1=C2C(OCCCO2)=CC(CN(CC(C)C)C([C@H]3CN(CC3)CC4=CC(OC)=C(C=C4)F)=O)=C1

Molecular Formula

C27H34ClFN2O4

Molecular Weight

505.02

References & Citations

[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.