MedChemExpress - Model PKRA83 - 1233926-87-8

FromMedChemExpress LLC (MCE)

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].

PKRA83

MCE China：PKRA83

Brand：MedChemExpress (MCE)

Cat. No.HY-147056

CAS：1233926-87-8

Synonyms：PKRA7

Purity：98.04%

Storage：Pure form -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

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, anti-arthritis and anti-angiogenic activities. PKRA83 can penetrate the blood-brain barrier.

In Vitro：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].

In Vivo：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].

IC50 & Target：IC50: 5.0 nM (PKR1) and 8.2 nM (PKR2)[1] In Vitro 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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PKRA83 Related Antibodies

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

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