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别名 | Galardin | 储存条件 (自收到货起) |
3年 / -20°C / 粉状 1年 / -80°C / 溶于溶剂 |
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化学式 | C20H28N4O4 |
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分子量 | 388.46 | CAS号 | 142880-36-2 | |
Solubility (25°C)* | 体外 | DMSO | 78 mg/mL (200.79 mM) | |
Ethanol | 4 mg/mL (10.29 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
产品描述 | Ilomastat (GM6001)是一种广谱matrix metalloprotease (MMP)(基质金属蛋白酶)抑制剂,作用于MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14,和MMP-26,Ki分别为0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM,和0.36 nM。 | |||||||||||
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靶点 |
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体外研究 | GM6001抑制人皮肤成纤维胶原酶,当用合成硫代酯底物在pH 6.5下测试时,Ki为0.4 nM,选择性比两种生物酶,嗜热菌蛋白酶和绿脓杆菌弹性蛋白酶高50倍。[1] GM 6001 (0.1 nM - 10 nM)抑制T细胞产生明胶酶A和明胶酶B,从而抑制T细胞归巢。[2] |
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体内研究 | GM6001 (400 微克/毫升)的局部使用可以预防严重碱烧伤后角膜溃疡。[3] 植入支架的兔子模型中,GM6001显著抑制内膜增生和内层胶原蛋白含量,并且它增加扩张动脉的管腔面积,而不影响增值率。[4] |
激酶实验 | 胶原酶测试 | |
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胶原酶测定使用合成硫羟酸酯底物Ac-Pro-Leu-Gly-SCH(i-Bu)CO-Leu-Gly-OEt在pH 6.5下进行。胶原酶浓度为1-2 nM,基底浓度为0.1 到 0.7 nM。Km在1.5到4 mM之间变化。 | ||
动物实验 | 动物模型 | Rabbit |
剂量 | 100 毫克/千克/天 | |
给药处理 | 皮下注射 |
, Mol Cancer, 2015, 14(1):83.
数据来源于[Data independently produced by , , J Biol Chem, 2016, 291(44):22977-22987]
数据来源于[Data independently produced by , , Sci Rep, 2015, 5:16951]
数据来源于[Data independently produced by , , Am J Physiol Lung Cell Mol Physiol, 2018, 314(5):L695-L707]
Signaling via a CD27-TRAF2-SHP-1 axis during naive T cell activation promotes memory-associated gene regulatory networks [ Immunity, 2024, 57(2):287-302.e12] | PubMed: 38354704 |
Cholinergic signaling via muscarinic M1 receptor confers resistance to docetaxel in prostate cancer [ Cell Rep Med, 2024, 5(2):101388] | PubMed: 38262412 |
Driving role of head and neck cancer cell secretome on the invasion of stromal fibroblasts: Mechanistic insights by phosphoproteomics [ Biomed Pharmacother, 2023, 158:114176] | PubMed: 36916400 |
Extracellular vesicles from human urine-derived stem cells delay aging through the transfer of PLAU and TIMP1 [ Acta Pharmaceutica Sinica B, 2023, 10.1016/j.apsb.2023.12.009] | PubMed: none |
Cell-matrix interface regulates dormancy in human colon cancer stem cells [ Nature, 2022, 10.1038/s41586-022-05043-y] | PubMed: 35798028 |
Targeting matrix metallopeptidase 2 by hydroxyurea selectively kills acute myeloid mixed-lineage leukemia [ Cell Death Discov, 2022, 8(1):180] | PubMed: 35396375 |
Complete abrogation of key osteoclast markers with a membrane-anchored tissue inhibitor of metalloproteinase : a novel approach in the prevention of osteoclastogenesis [ Bone Joint Res, 2022, 11(11):763-776] | PubMed: 36331083 |
Dynamic Alteration in HLA-E Expression and Soluble HLA-E via Interaction with Natural Killer Cells in Gastric Cancer [ Ann Surg Oncol, 2022, 10.1245/s10434-022-12505-0] | PubMed: 36149610 |
A potent tumor-selective ERK pathway inactivator with high therapeutic index [ PNAS Nexus, 2022, 1(3):pgac104] | PubMed: 35899070 |
Macrophage depletion induces edema through release of matrix-degrading proteases and proteoglycan deposition [ Sci Transl Med, 2021, 13(598)eabd4550] | PubMed: 34135110 |
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如果需要长期保存,请于零下二十度低温保存。禁止用于人体及治疗!
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