150113-99-8Decanoyl-RVKR-CMK

产品属性：

Cas No.150113-99-8

别名 Furin Inhibitor I

化学名 (2S,5R,8R,11S)-5-(4-aminobutyl)-2,11-bis(3-((diaminomethylene)amino)propyl)-8-isopropyl-4,7,10,13-tetraoxo-3,6,9,12-tetraazatricosan-1-oyl chloride

分子式 C34H66ClN11O5

分子量 744.42

溶解度 33mg/mL in ethanol, or in DMSO, or in DMF

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
Furin is a proprotein convertase, converting precursor proteins to functional proteins within the Golgi/trans-Golgi secretory pathway. Furin inhibitor I is a selective, irreversible, and cell-permeable competitive inhibitor of proprotein convertases, including furin/SPC1 (Ki = ~1 nM), SPC2/PC2 (Ki = 0.36 nM), SPC3/PC1/PC3 (Ki = 2.0 nM), SPC4/PACE4 (Ki = 3.6 nM), SPC6/PC5/PC6, and SPC7/LPC/PC7/PC8 (Ki = 0.12 nM).[1],[2] Because furin activates viral glycoproteins, this inhibitor is a useful antiviral agent.[3] In addition, it inhibits furin-dependent pro-MMP-2 activation in mononuclear inflammatory cells.[4]

Reference:

[1]. Angliker, H., Wikstrom, P., Shaw, E., et al. The synthesis of inhibitors for processing proteinases and their action on the Kex2 proteinase of yeast. Biochemistry Journal 293(1), 75-81 (1993).

[2]. Fugère, M., Limperis, P.C., Beaulieu-Audy, V., et al. Inhibitory potency and specificity of subtilase-like Pro-protein convertase (SPC) prodomains. The Journal of Biological Chemisty 277(10), 7648-7656 (2002).

[3]. Wanyiri, J.W., O'Connor, R., Allison, G., et al. Proteolytic processing of the Cryptosporidium glycoprotein gp40/15 by human furin and by a parasite-derived furin-like protease activity. Infection and Immunity 75(1), 184-192 (2007).

[4]. Stawowy, P., Meyborg, H., Stibenz, D., et al. Furin-like proprotein convertases are central regulators of the membrane type matrix metalloproteinase-pro-matrix metalloproteinase-2 proteolytic cascade in atherosclerosis. Circulation 111(21), 2820-2827 (2005).