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

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.

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A-176120 Chemical Structure

A-176120 Chemical Structure

CAS No. : 185049-54-1

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Description

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].

Molecular Weight

583.58

Formula

C33H29NO9

CAS No.
SMILES

O=C(C1=CC(C(N(CC2=CC=CC=C2OCC)CC3=CC=CC(OC4=CC=C(C)C=C4)=C3)=O)=C(C(O)=O)C=C1C(O)=O)O

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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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A-176120
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HY-117807
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