Stibogluconatesodium是蛋白酪氨酸磷酸酶(phosphatase)的有效抑制剂。Stibogluconatesodium在10，100和100μg/mL时分别抑制99%的SHP-1，SHP-2和PTP1B活性。
CAS：16037-91-5
分子式：C12H38Na3O26Sb2
分子量：910.9
纯度：98%
存储：Store at -20°C

Background:

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.

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].

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].

[1]. Pathak MK, et al. Sodium stibogluconate is a potent inhibitor of protein tyrosine phosphatases and augments cytokine responses in hemopoietic cell lines. J Immunol. 2001 Sep 15;167(6):3391-7. [2]. Fan K et al. Sodium Stibogluconate Interacts with IL-2 in Anti-Renca Tumor Action via a T Cell-Dependent Mechanism in Connection with Induction of Tumor-Infiltrating Macrophages. J Immunol. 2005 Nov 15;175(10):7003-8.