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Prokineticin 2 Antagonist, PKRA7-Calbiochem

品牌
Sigma-Aldrich
货号
5.08942
规格纯度
A cell permeable, brain permeant antagonist of polypeptide chemokine prokineticin 2 receptor (IC50 = 5 nM and 8.2 nM for PKR1 and PKR2, respectively).
参考价格
2780.86 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

一般描述

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.
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.

生化/生理作用

Primary Target
PROK2
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

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

法律信息

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

基本信息

经验(实验)分子式C27H34ClFN2O4
分子量505.02

产品性质

质量水平100
测定≥98% (HPLC)
形式semisolid
效能5 nM IC50
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 colorless
溶解性DMSO: 100 mg/mL
储存温度2-8℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

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