Merck, 521000-250MG, Phenylarsine Oxide

General description
A membrane-permeable phosphotyrosine phosphatase inhibitor (IC₅₀ = 18 µM). Stimulates 2-deoxyglucose transport in insulin-resistant human skeletal muscle and activates P56lck protein tyrosine kinase. Blocks TNFα-dependent activation of the NF-κB in human myeloid ML-1a cells. PAO inhibits the protease activities of recombinant human caspases, as well as endogenous chicken caspases that are active in extracts of preapoptotic chicken DU249 cells (S/M extracts). At 100 µM, it also blocks the morphological changes of nuclear apoptosis in vitro and internucleosomal DNA fragmentation in S/M extracts without interfering with PARP or lamin A cleavage. Also known to cause complete and reversible inhibition of NADPH oxidase in human neutrophils.
A membrane-permeable protein tyrosine phosphatase inhibitor (IC₅₀ = 18 µM). Stimulates 2-deoxyglucose transport in insulin-resistant human skeletal muscle and activates p56lck protein tyrosine kinase. Blocks TNF-α-dependent activation of NF-κB in human myeloid ML-1a cells. PAO inhibits the protease activities of recombinant human caspases as well as endogenous caspases that are active in extracts of pre-apoptotic chicken DU249 cells (S/M extracts).
Biochem/physiol Actions
Primary Target
Protein tyrosine phosphatase
Target IC₅₀: 18 µM against protein tyrosine phosphatase
Preparation Note
Following reconstitution, aliquot and freeze at -20°C. Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Takahashi, A., et al. 1997. Exp. Cell Res.231, 123.
Carey, J.O., et al. 1995. Diabetes44, 1995.
Le Cabec, V., and Maridonneau-Parini, I. 1995. J. Biol. Chem.270, 2067.
Oetken, C., et al. 1995. Mol. Immunol.31, 1295.
Singh, S., and Aggarwal, B.B. 1995. J. Biol. Chem.270, 10631.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Highly Toxic & Carcinogenic / Teratogenic (I)