货号:A237914 同义名: GM6001;Galardin
Ilomastat(GM6001) 是一种高效的广谱基质金属蛋白酶 (MMP) 抑制剂,对 MMP-1、MMP-2、MMP-3 和 MMP-9 的 IC50 值分别为 1.5 nM、1.1 nM、1.9 nM 和 0.5 nM,对人皮肤成纤维细胞胶原酶 (MMP-1) 的 Ki 为 0.4 nM。
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产品名称 | MMP ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Marimastat |
+++
MMP-14, IC50: 3 nM MMP-7, IC50: 16 nM |
98% | |||||||||||||||||
Ilomastat |
++++
MMP-2, Ki: 0.1 nM MMP-26, Ki: 0.36 nM |
99%+ | |||||||||||||||||
SB-3CT |
+
MMP-2, Ki: 13.9 nM MMP-9, Ki: 600 nM |
99%+ | |||||||||||||||||
Doxycycline | ✔ | 98% | |||||||||||||||||
Batimastat |
+++
MMP-7, IC50: 4 nM MMP-1, IC50: 3 nM |
99%+ | |||||||||||||||||
Nobiletin | ✔ | 98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | GM 6001 is a broad spectrum MMP inhibitor with Ki values of 0.1nM, 0.2nM, 0.36nM, 0.4nM, 0.5nM, 3.6nM and 3.7nM for MMP-8, MMP-9, MMP-26, MMP-1, MMP-2, MMP-12 and MMP-7[1]. The tyrosine phosphorylation of EGFR induced by leptin could be significantly attenuated by treatment with 25μM GM6001 for 30min in rat aortic smooth muscle cells, due to the inhibition of proteolytic cleavage of transmembrane precursors via matrix metalloproteinase by GM6001[2]. Inhibition of MMP-2/MMP-9-mediated NCAM (Neural cell adhesion molecule) proteolysis by administration of 5μg GM6001 through intracerebroventricular route 30 minutes before and 2 h after ischemia attenuated the infarction, behavioral abnormalities of MCAO (middle cerebral artery occlusion) model mice, with suppression on the level of NCAM cleavage product by GM6001 observed[3]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
HEk293 cells | Function assay | Inhibition of human recombinant ADAMTS4 expressed in HEk293 cells using FAM-AEwLQGRPISIAK-TAMRA as substrate measured for 15 mins by fluorometric analysis, IC50=0.48 μM | 23376997 | ||
human U251 cells | 20 μM | Function assay | Protection against anthrax PA63-lethal toxin complex-induced cytotoxicity in human U251 cells at 20 uM at 400 ng/ml by MTT test | 17537721 |
Dose | Hamster: 20 mg/kg[4] (i.p.) Rat: 1.2 mg/kg[5] (i.p.); 50 mg/kg, 100 mg/kg[6] (i.p.) |
Administration | i.p. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03297827 | - | Recruiting | August 27, 2019 | United States, New Mexico ... 展开 >> Department of Neurology, University of New Mexico Recruiting Albuquerque, New Mexico, United States, 87131-0007 Contact: Asad Ikram, MD 505-272-9382 aikram@salud.unm.edu Principal Investigator: Atif Zafar, MD Sub-Investigator: Asad Ikram, MD 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.57mL 0.51mL 0.26mL |
12.87mL 2.57mL 1.29mL |
25.74mL 5.15mL 2.57mL |
CAS号 | 142880-36-2 |
分子式 | C20H28N4O4 |
分子量 | 388.461 |
别名 | GM6001;Galardin |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,2-8°C |
溶解度 |
DMSO: 45 mg/mL(115.84 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
2% DMSO+40% PEG 300+2% Tween 80+water 11 mg/mL |