受注:045-509-1970 |
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Synonyms | Galardin | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C20H28N4O4 |
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分子量 | 388.46 | CAS No. | 142880-36-2 | ||||||||||||
Solubility (25°C)* | 体外 | DMSO | 78 mg/mL (200.79 mM) | ||||||||||||
Ethanol (warmed with 50ºC water bath) | 8 mg/mL (20.59 mM) | ||||||||||||||
Water | Insoluble | ||||||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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. |
製品説明 | Ilomastat (GM6001) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 0.36 nM, respectively. |
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in vitro | GM6001 inhibits human skin fibroblast collagenase with Ki of 0.4 nM when assayed with a synthetic thio ester substrate at pH 6.5, with 50-fold selectivity over two bacterial enzymes, thermolysin and Pseudomonas aeruginosa elastase. [1] GM 6001 (0.1 nM - 10 nM) inhibits gelatinase A and gelatinase B produced by T-cells, thus inhibits T-cell homing. [2] |
in vivo | Topical application of GM6001 (400 μg/ml) prevents corneal ulceration after severe alkali injury. [3] In rabbit model after stenting, GM6001 significantly inhibits intimal hyperplasia and intimalcollagen content, and it increases lumen area in stented arteries without effects on proliferation rates. [4] |
キナーゼアッセイ | Collagenase assay | |
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Collagenase assay uses the synthetic thiol ester substrate Ac-Pro-Leu-Gly-SCH(i-Bu)CO-Leu-Gly-OEt at pH 6.5. The collagenase concentration is 1-2 nM, and the substrate concentrations are from 0.1 to 0.7 nM. Km is found to vary between 1.5 and 4 mM. | ||
細胞アッセイ | 細胞株 | MLL cells |
濃度 | 20 µM | |
反応時間 | 72 h | |
実験の流れ | Cell viability was measured after 72-h exposure to triapine with co-treatment of 20 µM ilomastat |
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動物実験 | 動物モデル | Rabbit |
投薬量 | 100 mg/kg/day | |
投与方法 | subcutaneous |
, , Mol Cancer, 2015, 14(1):83.
Data from [Data independently produced by , , J Biol Chem, 2016, 291(44):22977-22987]
Data from [Data independently produced by , , Sci Rep, 2015, 5:16951]
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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。