PKRA83(Synonyms: PKRA7)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

PKRA83 (Synonyms: PKRA7)

PKRA83 (PKRA7) 是一种有效的促动力 (PK2) 拮抗剂,可竞争 PK2 与其受体 PKR1 和 PKR2 的结合。PKRA83 有效抑制 PK2 受体,对 PKR1 和 PKR2 的 IC50 值分别为 5.0 nM 和 8.2 nM。PKRA83 具有抗癌和抗血管生成活性。 PKRA83 可以穿透血脑屏障。

PKRA83(Synonyms: PKRA7)

PKRA83 Chemical Structure

CAS No. : 1233926-87-8

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生物活性

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].

IC50 & Target

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

体外研究
(In Vitro)

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

505.02

Formula

C27H34ClFN2O4

CAS 号

1233926-87-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [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.

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