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N-Acetyl-S-farnesyl-L-cysteine

Methyltransferase inhibitor
 
BML-G200-0005 5 mg 105.00 USD
 
BML-G200-0025 25 mg 409.00 USD
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Replaces Prod. #: ALX-290-001

Members of the Ras superfamily of G proteins, γ-subunits of heterotrimeric G proteins and the α-subunit of cGMP phosphodiesterase from retinal rods are all carboxyl methylated at carboxy-terminal S-farnesylcysteine residues. AFC specifically inhibits the S-farnesylcysteine methyl transferase (Km=20 µM) in cell free extracts and in whole cells. It inhibits carboxyl methylation of p21ras platelet Rap15 and the γ-subunit of transducin. It blocks receptor-mediated signal transduction in platelets and neutrophils not by inhibiting the methyltransferase, but possibly by inhibiting capacitative Ca2+ entry.

Product Details

Alternative Name:AFC
 
Formula:C20H33NO3S
 
MW:367.5
 
Source:Synthetic.
 
CAS:135304-07-3
 
Purity:≥98% (HPLC)
 
Appearance:Pale yellow oil.
 
Solubility:Soluble in DMSO (25mg/ml), methanol or 100% ethanol (25mg/ml).
 
Shipping:Ambient Temperature
 
Long Term Storage:-20°C
 
Handling:Keep under inert gas. Protect from light.
 
Regulatory Status:RUO - Research Use Only
 
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Product Literature References

Role of phosphatase activity of soluble epoxide hydrolase in regulating simvastatin-activated endothelial nitric oxide synthase: H. Hou, et al.; Sci. Rep. 5, 13524 (2015), Application(s): Cell culture, Abstract;
Inhibition of capacitative Ca2+ entry into cells by farnesylcysteine analogs: Y. Xu, et al.; Mol. Pharmacol. 50, 1495 (1996), Abstract;
Farnesyl-L-cysteine analogs can inhibit or initiate superoxide release by human neutrophils: J. Ding, et al.; J. Biol. Chem. 269, 16837 (1994), Abstract;
Carboxyl methylation of Ras-related proteins during signal transduction in neutrophils: M.R. Philips, et al.; Science 259, 977 (1993), Abstract;
Protein prenylcysteine analog inhibits agonist-receptor-mediated signal transduction in human platelets: A. Huzoor, et al.; PNAS 90, 868 (1993), Abstract;
Effects of farnesylcysteine analogs on protein carboxyl methylation and signal transduction: C. Volker, et al.; J. Biol. Chem. 266, 21515 (1991), Abstract;