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GW 280264X
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GW 280264X图片
CAS NO:866924-39-2
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
GW 280264X 是混合的 ADAM10/TACE (ADAM17) 金属蛋白酶抑制剂。
Cas No.866924-39-2
别名((S)-5-((2R,3S)-3-(N-羟基甲酰胺基)-2-异丁基六氨基)-2-氧代-6-(噻唑-2-基氨基)己基)氨基甲酸苄酯
Canonical SMILESO=CN(O)[C@@H](CCC)[C@@H](CC(C)C)C(N[C@@H](CCCCNC(OCC1=CC=CC=C1)=O)C(NC2=NC=CS2)=O)=O
分子式C28H41N5O6S
分子量575.7
溶解度DMSO: soluble
储存条件-20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

GW 280264X is an inhibitor of disintegrin and metalloproteinase domain-containing protein 17/TNF-α converting enzyme (ADAM17/TACE) and ADAM10 (IC50s = 8 and 11.5 nM, respectively).1It inhibits TNF-α-induced cleavage of endomucin in human umbilical vein endothelial cells (HUVECs) when used at a concentration of 10 µM.2GW 280264X (1 and 10 µM) inhibits angiotensin-converting enzyme 2 (ACE2) ectodomain shedding induced by phorbol 12-myristate 13-acetate in HEK-ACE2 cells.3It reduces ACE2 shedding and prevents severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection in HK-2 cells.4

1.Hundhausen, C., Misztela, D., Berkout, T.A., et al.The disintegrin-like metalloproteinase ADAM10 is involved in constitutive cleavage of CX3CL1 (fractalkine) and regulates CX3CL1-mediated cell-cell adhesionBlood102(4)1186-1195(2003) 2.Yang, J., LeBlanc, M.E., Cano, I., et al.ADAM10 and ADAM17 proteases mediate proinflammatory cytokine-induced and constitutive cleavage of endomucin from the endothelial surfaceJ. Biol. Chem.295(19)6641-6651(2020) 3.Lambert, D.W., Yarski, M., Warner, F.J., et al.Tumor necrosis factor-alpha convertase (ADAM17) mediates regulated ectodomain shedding of the severe-acute respiratory syndrome-coronavirus (SARS-CoV) receptor, angiotensin-converting enzyme-2 (ACE2)J. Biol. Chem.280(34)30113-30119(2005) 4.Yeung, M.L., Teng, J.L.L., Jia, L., et al.Soluble ACE2-mediated cell entry of SARS-CoV-2 via interaction with proteins related to the renin-angiotensin systemCell1841-17(2021)