| Bioactivity | 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[1][2][3]. | ||||||||||||
| Target | Cbl | ||||||||||||
| Invitro | Hydrocotarnine is an analgesic agent (CRIN-2), with the patent ID of WO2011160016A2[1].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[1]. Hydrocotarnine (50 μM; 0-100 min) increases the glycolytic capacity and glycolytic reserve capacity in THP-1-derived macrophages[2].Hydrocotarnine (50 μM; 16 h) inhibits Cbl and increases the total GLUT1 protein in THP-1-derived macrophages[2].Hydrocotarnine is known to enhance the analgesic effect of opioids, and alleviates cancer pain[3]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| 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[1].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[1]. Animal Model: | ||||||||||||
| Name | Hydrocotarnine | ||||||||||||
| CAS | 550-10-7 | ||||||||||||
| Formula | C12H15NO3 | ||||||||||||
| Molar Mass | 221.25 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [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, et al. DITMD-induced mitotic defects and apoptosis in tumor cells by blocking the polo-box domain-dependent functions of polo-like kinase 1. Eur J Pharmacol. 2019 Mar 15;847:113-122. |
Hydrocotarnine
CAS: 550-10-7 F: C12H15NO3 W: 221.25
Hydrocotarnine is a Cbl inhibitor, and results in inflammasome-mediated IL-18 secretion in colitis. Hydrocotarnine incre
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