1. GPCR/G Protein MAPK/ERK Pathway Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK
  2. Ras Farnesyl Transferase VEGFR
  3. A-176120

A-176120 是基于法呢基焦磷酸 (FPP) 类似物的法呢基转移酶 (Farnesyl Transferase) 的选择性抑制剂 (IC50=1.2 nM),高于对香叶基香叶基转移酶 GGTaseI (IC50=423 nM)、香叶基香叶基转移酶 GGTaseII (IC50=3000 nM) 和角鲨烯合酶 SSase (IC50>10 μM) 的选择性。 A-176120 抑制 H-ras 转化的 NIH3T3 细胞和 HCT116 K-ras 突变细胞中的 ras 加工 (ED50 分别为 1.6 和 0.5 μM)。A-176120 具有抗血管生成和体内抗肿瘤活性,可减少毛细血管结构形成,VEGF 分泌。

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A-176120

A-176120 Chemical Structure

CAS No. : 185049-54-1

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生物活性

A-176120 is a selective inhibitor of farnesyl transferase (IC50=1.2 nM) based on a farnesyl pyrophosphate (FPP) analog, with superior selectivity against GGTaseI (IC50=423 nM), GGTaseII (IC50=3000 nM), and SSase (IC50>10 μM). A-176120 inhibits ras processing in H-ras transformed NIH3T3 cells and HCT116 K-ras mutant cells (ED50=1.6 and 0.5 μM, respectively). A-176120 has antiangiogenic and antitumor activities in vivo and reduces capillary structure formation and VEGF secretion[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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  • 稀释计算器

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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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