1. Metabolic Enzyme/Protease
  2. Phosphatase

Stibogluconate sodium (Synonyms: Sodium stibogluconate)

Cat. No.: HY-100595 Purity: >98.0%
Handling Instructions

Stibogluconate sodium is a potent inhibitor of protein tyrosine phosphatase. Stibogluconate sodium inhibits 99% of SHP-1, SHP-2 and PTP1B activity at 10, 100, 100 μg/mL, respectively.

For research use only. We do not sell to patients.
Stibogluconate sodium Chemical Structure

Stibogluconate sodium Chemical Structure

CAS No. : 16037-91-5

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in Water USD 73 In-stock
500 mg USD 66 In-stock
1 g USD 96 In-stock
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Stibogluconate sodium is a potent inhibitor of protein tyrosine phosphatase. Stibogluconate sodium inhibits 99% of SHP-1, SHP-2 and PTP1B activity at 10, 100, 100 μg/mL, respectively.

IC50 & Target

Phosphatase[1]

In Vitro

Stibogluconate sodium inhibits 99% of SHP-1 activity at 10 μg/mL, a therapeutic concentration of the drug for leishmaniasis. Similar degrees of inhibition of SHP-2 and PTP1B required 100 μg/mL Stibogluconate sodium. The inhibition of cellular PTPases by the Stibogluconate sodium is suggested by its rapid induction of tyrosine phosphorylation of cellular proteins in Baf3 cells and its augmentation of IL-3-induced Janus family kinase 2/Stat5 tyrosine phosphorylation and proliferation of Baf3 cells. The augmentation of the opposite effects of GM-CSF and IFN-α on TF-1 cell growth by Stibogluconate sodium indicate its broad activities in the signaling of various cytokines[1].

In Vivo

Stibogluconate sodium induces 61% growth inhibition of Renca tumors in BALB/c mice coincident with an increase (2-fold) in tumor-infiltrating macrophages. A combination of Stibogluconate sodium and IL-2 is more effective in inhibiting tumor growth (91%) and inducing tumor-infiltrating (4-fold), whereas IL-2 alone has little effect[2].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.0978 mL 5.4891 mL 10.9782 mL
5 mM 0.2196 mL 1.0978 mL 2.1956 mL
10 mM 0.1098 mL 0.5489 mL 1.0978 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

Human myeloid cell line TF-1 is maintained in RPMI 1640 supplemented with 10% FCS and 40 ng/mL recombinant human GM-CSF. For cell proliferation assays, cells are washed in 10% FCS medium twice, resuspended in 10% FCS medium, incubated at 37°C for 16 h, and then cultured at 37°C in 10% FCS medium containing various amounts of cytokines, sodium stibogluconate, or potassium antimonyl tartrate for 3-6 days. The cell numbers in proliferation assays are determined by an MTT assay or by microscopic cell counting[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

BALB/c and athymic nude BALB/c mice are inoculated (s.c.) at the flanks with Renca cells (106 cells/site). Four days after inoculation, the mice are subjected to no treatment (control) or treatment with IL-2 (105 IU/day for 5 days i.p.), Stibogluconate sodium (12 mg/day i.m. at hip regions), or the combination of the two agents for 2 wk. Tumor volume is measured during the study period and calculated using the formula for a prolate spheroid[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

910.9

Formula

C₁₂H₃₈Na₃O₂₆Sb₂

CAS No.

16037-91-5

SMILES

O=[Sb](O[[email protected]]1([H])[[email protected]](O)CO)(O[[email protected]@H](C(O)=O)[[email protected]]1O)O[Sb](O[[email protected]]2([H])[[email protected]](O)CO)(O[[email protected]@H](C(O)=O)[[email protected]]2O)=O.[9H2O].[3Na]

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

H2O: 550 mg/mL (Need warming); DMSO: < 9.1 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: >98.0%

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Product Name:
Stibogluconate sodium
Cat. No.:
HY-100595
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