Sodium stibogluconate 是一种有效的蛋白酪氨酸磷酸酶 (Phosphatase) 抑制剂。 它在10,100 和 100 μg/mL 时分别抑制 99% 的 SHP-1,SHP-2 和 PTP1B 活性。
产品描述
Sodium stibogluconate is a potent protein tyrosine phosphatase inhibitor.
体外活性
99% of SHP-1 activity at 10 μg/mL inhibited by Sodium stibogluconate. Similar degrees of inhibition of SHP-2 and PTP1B required 100 μg/mL Sodium stibogluconate. The inhibition of cellular PTPases by the Sodium stibogluconate 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 Sodium stibogluconate indicate its broad activities in the signaling of various cytokines[1].
体内活性
Sodium stibogluconate induces 61% growth inhibition of Renca tumors in BALB/c mice coincident with an increase (2-fold) in tumor-infiltrating macrophages. A combination of Sodium stibogluconate and IL-2 is more effective in inhibiting tumor growth (91%) and inducing tumor-infiltrating (4-fold)[2].
Cas No.
16037-91-5
分子式
C12H22NaO18Sb2
分子量
720.8
别名
葡萄糖酸锑钠;Stibogluconate trisodium nonahydrate
储存和溶解度
H2O:6.67 mg/mL (7.32 mM),ultrasonic and adjust pH to 3 with 1M HCl
DMSO:< 1 mg/mL (insoluble or slightly soluble)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years