Ilomastat (GM6001)

製品コードS7157 バッチS715703

印刷

化学情報

Chemical Structure Synonyms Galardin Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H28N4O4
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) 4 mg/mL (10.29 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 2.500mg/ml (6.44mM) Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Ilomastat (GM6001)は、MMP-1、MMP-2、MMP-3、MMP-7、MMP-8、MMP-9、MMP-12、MMP-14、およびMMP-26に対する広範囲のマトリックスメタロプロテアーゼ (MMP)阻害剤であり、それぞれKiは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です。
in vitro

Ilomastat (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.

This compound (0.1 nM - 10 nM) inhibits gelatinase A and gelatinase B produced by T-cells, thus inhibits T-cell homing.

in vivo

Topical application of Ilomastat (GM6001) (400 μg/ml) prevents corneal ulceration after severe alkali injury.

In rabbit model after stenting, it significantly inhibits intimal hyperplasia and intimalcollagen content, and increases lumen area in stented arteries without effects on proliferation rates.

プロトコル(参考用のみ)

キナーゼアッセイ Collagenase assay
Ilomastat (GM6001) is assayed using 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 (GM6001)
動物実験 動物モデル Rabbit
投薬量 100 mg/kg/day
投与方法 subcutaneous

参考

  • https://pubmed.ncbi.nlm.nih.gov/1322694/
  • https://pubmed.ncbi.nlm.nih.gov/7722295/
  • https://pubmed.ncbi.nlm.nih.gov/1385350/
  • https://pubmed.ncbi.nlm.nih.gov/12039502/
  • https://pubmed.ncbi.nlm.nih.gov/35396375/

カスタマーフィードバック

, , 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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Sos1 ablation alters focal adhesion dynamics and increases Mmp2/9-dependent gelatinase activity in primary mouse embryonic fibroblasts [ Cell Commun Signal, 2025, 23(1):116] PubMed: 40033301
Mesenchymal Stem Cells Restore Endothelial Integrity and Alleviate Emotional Impairments in a Diabetic Mouse Model via Inhibition of MMP-9 Activity [ Int J Mol Sci, 2025, 26(7)3355] PubMed: 40244194
Inhibition of matrix metalloproteinase-9 attenuates kidney fibrosis and cellular senescence in the transition from acute kidney injury to chronic kidney disease [ Ren Fail, 2025, 47(1):2499897] PubMed: 40468751
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
Extracellular vesicles from human urine-derived stem cells delay aging through the transfer of PLAU and TIMP1 [ Acta Pharm Sin B, 2024, 14(3):1166-1186] PubMed: 38487008
Cholinergic signaling via muscarinic M1 receptor confers resistance to docetaxel in prostate cancer [ Cell Rep Med, 2024, 5(2):101388] PubMed: 38262412
Epithelial tubule interconnection driven by HGF-Met signaling in the kidney [ Proc Natl Acad Sci U S A, 2024, 121(52):e2416887121] PubMed: 39705305
ADAMTS2 promotes radial migration by activating TGF-β signaling in the developing neocortex [ EMBO Rep, 2024, 25(7):3090-3115] PubMed: 38871984
Matrix metalloproteinases mediate influenza A-associated shedding of the alveolar epithelial glycocalyx [ PLoS One, 2024, 19(9):e0308648] PubMed: 39312544
Decanoylcarnitine Inhibits Triple-Negative Breast Cancer Progression via Mmp9 in an Intermittent Fasting Obesity Mouse [ Technol Cancer Res Treat, 2024, 23:15330338241233443] PubMed: 38409962

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。