Merck, 567565-1GM, Sodium Stibogluconate

General description
A pentavalent antimony compound that forms a stable complex with and irreversibly inhibits Src homology protein tyrosine phosphatase (SHP-1) (99% inhibition at 11 µM). Also inhibits SHP-2 and PTP1B at an ~10-fold higher concentration (~110 µM). Does not inhibit the dual specificity protein tyrosine phosphatase (PTPase) or mitogen-activated protein kinase phosphatase-1 (MKP-1). Reported to induce general protein tyrosine phosphorylation and enhance IL-3-induced protein tyrosine phosphorylation of Jak2 and Stat5 in Baf3 cells. Also reported to augment IL-3-induced proliferation in Baf3 cells (ECmax = 44 µM) and GM-CSF-induced proliferation in TF-1 cells (ECmax = 55 µM). Exhibits anti-leishmanial effects.
A pentavalent antimony compound that irreversibly inhibits protein tyrosine phosphatase (PTPase) activity, including Src homology PTPase-1 (SHP-1) (99% inhibition at ~11 µM) by forming a stable complex. At higher concentrations (~110 µM), it inhibits SHP-2 and PTP1B activities.
Biochem/physiol Actions
Cell permeable: no
Primary Target
PTPase activity, including Src homology PTPase-1 (SHP-1)
Product does not compete with ATP.
Reversible: yes
Target IC₅₀: ~11 µM causing 99% inhibition of protein tyrosine phosphatase (PTPase) activity, including Src homology PTPase-1 (SHP-1)
Packaging
Packaged under inert gas
Preparation Note
Heating to 75°C with constant stirring or constant stirring overnight at room temperature may be required for complete solubilization.
Unstable in solution; reconstitute just prior to use.
Other Notes
Wortmann, G., et al. 2002. Clin. Infect. Dis.35, 261.
Pathak, M.K. and Yi, T. 2001. J. Immunol.167, 3391.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)