5-Iodotubercidin is a potent inhibitor (IC50 = 26 nM). It also inhibits nucleoside transporter, CK1,insulin receptor tyrosine kinase,phosphorylase kinase, PKA, CK2 and PKC.
5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin facilitates glycogen synthesis in isolated hepatocytes by deactivating phosphorylase and activating glycogen synthase. Furthermore, 5-Iodotubercidin obstructs the activity of several kinases including CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC, and Haspin[1].[2].[3].
体内研究
Additionally, 5-Iodotubercidin demonstrated effectiveness in combating bicuculline-induced seizures when administered locally into the prepiriform cortex at a dosage of 1 mL/kg, i.p., highlighting its potential therapeutic applications[2].
体外研究
5-Iodotubercidin (NSC 113939) has the inhibition specificity of 5-Iodotubercidin towards CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, and PKC is quantified by IC50 values of 0.4, 3.5, 5-10, 5-10, 10.9, and 27.7 μM, respectively[1].
At a concentration of 20 μM, 5-Iodotubercidin significantly reduces ATP levels while slightly increasing AMP levels. It also decreases the activity of acetyl-CoA carboxylase (ACC), leading to reduced synthesis of fatty acids and cholesterol. This is associated with a substantial drop in malonyl-CoA levels inside cells, a result of ACC inhibition by iodotubercidin[4].
作用机制
5-iodotubercidin increases the release of adenosine from hypoxic/hypoglycemic hippocampal slices[2].
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