| 货号 | 18505-5mg |
| 描述 | TNF-α converting enzyme (TACE, also known as ADAM17) is a zinc metalloprotease that cleaves the membrane-bound precursor of TNF-α to give the mature soluble form of TNF-α.1,2 It also mediates the proteolytic release of several other cell-surface proteins, including TNF-α receptors (TNFRs). TAPI-1, known in the earlier literature as just TAPI, is an inhibitor of TACE that inhibits the cleavage of TNF-α, TNFRI (p60), and TNFRII (p80) with IC50 values ranging from 5-100 µM.1,3,4 It also blocks the shedding of other TACE-dependent proteins, including IL-6R and Klotho, and may inhibit metalloproteases other than TACE.2,5,6 TAPI-1 differs from TAPI-0 (Item No. 14694), structurally, by the presence of an aminoethyl addition at the alanyl group, and is generally more stable in tissue culture and in vivo. |
| 别名 | TAPI; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Mohler, K.M.,Sleath, P.R.,Fitzner, J.N., et al. Protection against a lethal dose of endotoxin by an inhibitor of tumour necrosis factor processing. Nature 370(6486), 218-220 (1994). 2.Müllberg, J.,Durie, F.H.,Otten-Evans, C., et al. A metalloprotease inhibitor blocks shedding of the IL-6 receptor and the p60 TNF receptor. Journal of Immunology 155(11), 5198-5205 (1995). 3.Crowe, P.D.,Walter, B.N.,Mohler, K.M., et al. A metalloprotease inhibitor blocks shedding of the 80-kD TNF receptor and TNF processing in T lymphocytes. Journal of Experimental Medicine 181(3), 1502-1210 (1995). 4.Hooper, N.M.,Karran, E.H. and Turner, A.J. Membrane protein secretases. Biochemistry Journal 321(2), 265-279 (1997). 5.Chen, C.D.,Podvin, S.,Gillespie, E., et al. Insulin stimulates the cleavage and release of the extracellular domain of klotho by ADAM10 and ADAM17. Proceedings of the National Academy of Sciences of the United States of America 104(50), 19796-19801 (2007). 6.Yamamoto, K.,Miyazaki, K. and Higashi, S. Pericellular proteolysis by matrix metalloproteinase-7 is differentially modulated by cholesterol sulfate, sulfatide, and cardiolipin. FEBS Journal 281(15), 3346-3356 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 499.6 |
| 分子式 | C26H37N5O5 |
| CAS号 | 171235-71-5 |
| 稳定性 | ≥ 2 years |
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