Inxight Drugs

Oxophenylarsine (Phenylarsine oxide, PAO, PhAsO) is an organometallic compound with the phenyl group and an oxygen atom bonded to an arsenic atom. The arsenic atom in PAO has a high affinity for the sulfur atom of thiols inorganic compounds, in particular, forming stable complexes with vicinal cysteine residues in protein structures. This effect makes it the useful tool to investigate the interaction of peptides such as insulin with their receptors and the signal transduction from the receptor to the cell interior. Oxophenylarsine is commonly used in cell biological research as an inhibitor of phosphotyrosine phosphatases (PTPases); in particular, PTPases HA1, HA2, and SH-PTP2 have been identified as substrates for Oxophenylarsine. Covalent binding of Oxophenylarsine to cysteinyl residues residing in the catalytic sites causes inactivation of PTPases. Oxophenylarsine also acts on other phosphatases that harbor vicinal thiol groups [i.e., inositol 1,2,3,5,6-pentakisphosphate 5-phosphatase or calcineurin, a Ca2+/calmodulin-dependent serine/threonine phosphatase. Also, NADPH oxidase and mitochondrial adenine nucleotide transporter were reported to be inhibited by Oxophenylarsine. Furthermore, steric inhibition of Oxophenylarsine-linked NFκB was suggested to be responsible for its decreased binding to DNA.

MYRISTICIN

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04PD6CT78W

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CHEMICAL (ACHIRAL)

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Myristicin, a natural product found in nutmeg oil and nutmeg extract, contains the carbon skeleton for a series of drugs of abuse related to the 3,4-methylenedioxyamphetamines (MDAs). Myristicin, 1-(3-methoxy-4,5-methylenedioxyphenyl)-2-propene, was identified as the major component of commercially available nutmeg oil and in the organic extract of nutmeg powder. Myristicin, or methoxysafrole, is a benzodioxole with slight MAO-inhibiting properties. Myristicin is active at the 5-HT receptors in the brain, and has been shown to have hypotensive, sedative, anti-depressant, anesthetic, hallucinogenic, and serotonergic properties. Large doses generally cause hyper-excitability, followed by CNS depression. Myristicin has been shown to have potent anti-cancer properties. A 65% inhibition of the tumor multiplicity in the lung of rats was observed as the result of treatment of myristicin in rats. Myristicin showed a 31% inhibition of tumor formation in the forestomach of rats. Mice given 5 to 50 mg doses of myristicin, showed 4- to 14-fold increase in liver glutathione S-transferase (GST) activity.