Hydrocotarnine is a Cbl inhibitor, and results in inflammasome-mediated IL-18 secretion in colitis. Hydrocotarnine increases expression of GLUT1 and cellular glucose uptake in glycolytic metabolism. Hydrocotarnine acts as an agent that provides analgesic effect in cancer research.
性状
Solid
IC50 & Target[1][2]
Cbl
体外研究(In Vitro)
Hydrocotarnine is an analgesic agent (CRIN-2), with the patent ID of WO2011160016A2.Hydrocotarnine (10 μM; 1 h) elevates the secretion of IL-1β and IL-18, and (0.1-10 μM; 1 h) increases the global level of tyrosine-phosphorylated proteins in THP-1 cells. Hydrocotarnine (50 μM; 0-100 min) increases the glycolytic capacity and glycolytic reserve capacity in THP-1-derived macrophages.Hydrocotarnine (50 μM; 16 h) inhibits Cbl and increases the total GLUT1 protein in THP-1-derived macrophages.Hydrocotarnine is known to enhance the analgesic effect of opioids, and alleviates cancer pain. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Hydrocotarnine (10 mg/kg/d; i.p.; 9 d) shows inhibitory effect on Cbl and results in increasing IL-18 levels, indicating that NLRP3 inflammasome activation is enhanced in mice.
Hydrocotarnine (10 mg/kg/d; i.p.; 9 d) protects mice from DSS-induced colitis, with low scores of pathological evaluation of inflammation, epithelial defects, and crypt atrophy. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Chung IC, et al. Src-family kinase-Cbl axis negatively regulates NLRP3 inflammasome activation. Cell Death Dis. 2018 Oct 31;9(11):1109. [2]. Lin HC, et al. Cbl Negatively Regulates NLRP3 Inflammasome Activation through GLUT1-Dependent Glycolysis Inhibition. Int J Mol Sci. 2020 Jul 19;21(14):5104. [3]. Kim KU,