货号 | 14882-25g |
描述 | Tissue transglutaminase (TGM2) post-translationally modifies proteins by catalyzing intermolecular cross-linkages between glutamine and lysine side chains.1 TGM2 has roles in neurodegenerative disorders, celiac sprue, cancer, and fibrotic diseases.1,2 Cystamine is an organic disulfide that inhibits TGM2 with an IC50 value of approximately 2.5 mM.3 It is orally available and is neuroprotective in mouse models of Huntington’s disease.4,5 Cystamine also inhibits caspase 3, increases intracellular glutathione, and reduces inflammation in a rat model of inflammatory bowel disease.6 |
供应商 | Cayman |
应用文献 | |
1.Siegel, M. and Khosla, C. Transglutaminase 2 inhibitors and their therapeutic role in disease states. Pharmacology & Therapeutics 115(2), 232-245 (2007). 2.Caccamo, D.,Currò, M. and Ientile, R. Potential of transglutaminase 2 as a therapeutic target. Expert Opin.Ther.Targets 14(9), 989-1003 (2010). 3.Smethurst, P.A. and Griffin, M. Measurement of tissue transglutaminase activity in a permeabilized cell system: Its regulation by Ca2+ and nucleotides. Biochemistry Journal 131(pt3), 803-808 (1996). 4.Dedeoglou, A.,Kubilus, J.K.,Jeitner, T.M., et al. Therapeutic effects of cystamine in a murine model of Huntington’s disease. Journal of Neuroscience 22(20), 8942-8950 (2002). 5.Borrell-Pagès, M.,Canals, K.P.,Cordelièrs, F.P., et al. Cystamine and cysteamine increase brain levels of BDNF in Huntington disease via HSJ1b and transglutaminase. Journal of Clinical Investigation 116(5), 1410-1424 (2006). 6.Elli, L.,Ciulla, M.M.,Busca, G., et al. Beneficial effects of treatment with transglutaminase inhibitor cystamine on the severity of inflammation in a rat model of inflammatory bowel disease. Lab Invest. 91(3), 452-461 (2011). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 225.2 |
分子式 | C4H12N2S2 • 2HCl |
CAS号 | 56-17-7 |
稳定性 | ≥ 2 years |
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