| 货号 | 14533-500ug |
| 描述 | GM 6001 is a potent, reversible broad spectrum inhibitor of zinc-containing proteases, including matrix metalloproteinases (MMPs).1 It inhibits zinc-containing thermolysin and elastase from P. aeruginosa, both with Ki values of 20 nM.2 GM 6001 inhibits MMP-1, -2, -7, -8, -9, -12, -13, -14, -16, and -26 with Ki or IC50 values between 0.1 and 10 nM.3,4,5,6 It inhibits disintegrin and metalloproteinase domain-containing (ADAM) proteins ADAM9, ADAM10, ADAM12, and ADAM17 at nanomolar concentrations.7,8 It less potently inhibits lethal factor from B. anthracis anthrax lethal toxin (Ki = 2.74 μM).9 GM 6001 also impairs the growth of the human pathogen Chlamydia by inhibiting peptide deformylase, which contains iron rather than zinc (IC50 = 38 nM).10 |
| 别名 | Galardin;Ilomastat; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Augé, F.,Hornebeck, W.,Decarme, M., et al. Improved gelatinase a selectivity by novel zinc binding groups containing galardin derivatives. Bioorganic & Medicinal Chemistry Letters 13(10), 1783-1786 (2003). 2.Grobelny, D.,Poncz, L. and Galardy, R.E. Inhibition of human skin fibroblast collagenase, thermolysin, and Pseudomonas aeruginosa elastase by peptide hydroxamic acids. Biochemistry 31(3), 7152-7154 (1992). 3.Ma, D.,Wu, W.,Yang, G., et al. Tetrahydroisoquinoline based sulfonamide hydroxamates as potent matrix metalloproteinase inhibitors. Bioorganic & Medicinal Chemistry Letters 14(1), 47-50 (2004). 4.Levy, D.E.,Lapierre, F.,Liang, W., et al. Matrix metalloproteinase inhibitors: A structure-activity study. Journal of Medicinal Chemistry 41(2), 199-223 (1988). 5.Fray, M.J.,Burslem, M.F. and Dickinson, R.P. Selectivity of inhibition of matrix metalloproteases MMP-3 and MMP-2 by succinyl hydroxamates and their carboxylic acid analogues is dependent on P3 group chirality. Bioorganic & Medicinal Chemistry Letters 11(4), 567-570 (2001). 6.Yamamoto, M.,Tsujishita, H.,Hori, N., et al. Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket. Journal of Medicinal Chemistry 41(8), 1209-1217 (1998). 7.Oh, M.,Im, I.,Lee, Y.J., et al. Structure-based virtual screening and biological evaluation of potent and selective ADAM12 inhibitors. Bioorganic & Medicinal Chemistry Letters 14(24), 6071-6074 (2004). 8.Kwan, J.C.,Eksioglu, E.A.,Liu, C., et al. Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. Journal of Medicinal Chemistry 52(18), 5732-5747 (2009). 9.Kocer, S.S.,Walker, S.G.,Zerler, B., et al. Metalloproteinase inhibitors, nonantimicrobial chemically modified tetracyclines, and ilomastat block Bacillus anthracis lethal factor activity in viable cells. Infection and Immunity 73(11), 7548-7557 (2005). 10.Balakrishnan, A.,Patel, B.,Sieber, S.A., et al. Metalloprotease inhibitors GM6001 and TAPI-0 inhibit the obligate intracellular human pathogen Chlamydia trachomatis by targeting peptide deformylase of the bacterium. The Journal of Biological Chemisty 281(24), 16691-26696 (2006). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥90% |
| 计算分子量 | 388.5 |
| 分子式 | C20H28N4O4 |
| CAS号 | 142880-36-2 |
| 稳定性 | ≥ 2 years |
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