Ilomastat (GM6001)

Catalog No.S7157 Batch:S715702

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Technical Data

Formula

C20H28N4O4
Molecular Weight 388.46 CAS No. 142880-36-2
Solubility (25°C)* In vitro DMSO 78 mg/mL (200.79 mM)
Ethanol 8 mg/mL (20.59 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 95% Corn oil
3.4mg/ml Taking the 1 mL working solution as an example, add 50 μL of 68 mg/mL clarified DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
2% DMSO 40% PEG 300 2% Tween 80 ddH2O
11.0mg/ml Taking the 1 mL working solution as an example, add 20 μL of 550 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween-80 to the above system, mix evenly to clarify it; then continue adding Adjust the volume to 1 mL with 530 μL ddH2O. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG 300 5%Tween80 50% ddH2O
27.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 550 mg/mL clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify; add 50 μL Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description 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.
Targets
MMP-8 [1]
(Cell-free assay)		 MMP-9 [1]
(Cell-free assay)		 MMP-26 [1]
(Cell-free assay)		 MMP-1 [1]
(Cell-free assay)		 MMP-2 [1]
(Cell-free assay)		 View More
0.1 nM(Ki) 0.2 nM(Ki) 0.36 nM(Ki) 0.4 nM(Ki) 0.5 nM(Ki)
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]

Protocol (from reference)

Kinase Assay:

[1]
  • Collagenase assay

    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.
Cell Assay:

[5]
  • Cell lines

    MLL cells

  • Concentrations

    20 µM

  • Incubation Time

    72 h

  • Method

    Cell viability was measured after 72-h exposure to triapine with co-treatment of 20 µM ilomastat
Animal Study:

[4]
  • Animal Models

    Rabbit

  • Dosages

    100 mg/kg/day

  • Administration

    subcutaneous

Customer Product Validation

, , 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]

Data from [Data independently produced by , , Am J Physiol Lung Cell Mol Physiol, 2018, 314(5):L695-L707]

Selleck's Ilomastat (GM6001) has been cited by 52 publications

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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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.