1. GPCR/G Protein MAPK/ERK Pathway
  2. Ras
  3. A-176120

A-176120 是一种有效的法呢基转移酶抑制剂,对癌细胞中的 Ras 蛋白法呢基化至关重要。它对法呢基转移酶 (IC50 1.2 ± 0.3 nM) 的选择性高于香叶基香叶基转移酶和角鲨烯合酶等相关酶。抑制 H-rasK-ras 突变细胞中的 Ras 加工表明其在阻断 Ras 介导的信号传导方面有效。A-176120 通过抑制血管内皮生长因子 (VEGF) 分泌和破坏内皮细胞中的毛细血管形成,显示出抗血管生成作用。体内研究表明,它能够减少 Ras 转化细胞中的肿瘤生长并提高动物模型中的存活率。这些发现凸显了 A-176120 是一种有前途的 FPP 类似物,具有强大的抗肿瘤和抗血管生成特性。

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A-176120 Chemical Structure

A-176120 Chemical Structure

CAS No. : 185049-54-1

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生物活性

A-176120 is a potent inhibitor of farnesyltransferase, crucial for Ras protein farnesylation in cancer cells. It exhibits high selectivity for farnesyltransferase (IC50 1.2 ± 0.3 nM) over related enzymes like geranylgeranyltransferases and squalene synthase. Inhibition of Ras processing in H-ras and K-ras mutated cells demonstrates its efficacy in blocking Ras-mediated signaling. A-176120 shows anti-angiogenic effects by inhibiting vascular endothelial growth factor (VEGF) secretion and disrupting capillary formation in endothelial cells. In vivo studies reveal its ability to reduce tumor growth in Ras-transformed cells and enhance survival in animal models. These findings highlight A-176120 as a promising FPP analogue with potent anti-tumor and anti-angiogenic properties[1].

分子量

583.58

Formula

C33H29NO9

CAS 号
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.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
A-176120
目录号:
HY-117807
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