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Prokineticin 2 Antagonist, PKRA7-Calbiochem
| 产品编号： | 4083599 |
| 规格： | A cell permeable, brain permeant antagonist of polypeptide chemokine prokineticin 2 receptor (IC50 = 5 nM and 8.2 nM for PKR1 and PKR2, respectively). |
| 包装规格： | 5 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
Prokineticin 2 Antagonist, PKRA7-Calbiochem
PROK2 Antagonist, PKRA7, Bv8 Antagonist, PKRA7, PK2 Antagonist, PKRA7
基本信息
| Empirical Formula【经验(实验)分子式】 | C27H34ClFN2O4 |
| Molecular weight | 505.02 |
| General description【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. |
| Biochem/physiol Actions【生化/生理作用】 | Primary Target PROK2 Reversible: yes |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. |
| Other Notes【其他说明】 | Curtis, V., et al. 2013. PLoS One.8, e54916. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | semisolid |
| potency【效能】 | 5 nM IC50 |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | colorless |
| solubility【溶解性】 | DMSO: 100 mg/mL |
| storage temp.【储存温度】 | 2-8℃ |
| packaging【包装】 | Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
