Sodium Stibogluconate

Biochem/physiol Actions

Target IC₅₀: ~11 µM causing 99% inhibition of protein tyrosine phosphatase (PTPase) activity, including Src homology PTPase-1 (SHP-1)

Cell permeable: no

Reversible: yes

Product does not compete with ATP.

Primary TargetPTPase activity, including Src homology PTPase-1 (SHP-1)

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 (EC_max = 44 µM) and GM-CSF-induced proliferation in TF-1 cells (EC_max = 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Wortmann, G., et al. 2002. Clin. Infect. Dis.35, 261.Pathak, M.K. and Yi, T. 2001. J. Immunol.167, 3391.

Packaging

Packaged under inert gas

1 g in Plastic ampoule

Preparation Note

Heating to 75°C with constant stirring or constant stirring overnight at room temperature may be required for complete solubilization.

Reconstitution

Unstable in solution; reconstitute just prior to use.

Warning

Toxicity: Standard Handling (A)