Ilomastat (GM6001, Galardin)

Catalog No.S7157

Ilomastat (GM6001, Galardin) Chemical Structure

Molecular Weight(MW): 388.46

Ilomastat (GM6001, Galardin) 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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Cited by 15 Publications

5 Customer Reviews

  • GM6001 inhibits MMP-7 and −10 mRNA expressions in Aurora-A stable cells in HNC. The mRNA expression levels of MMP-7 and −10 were examined by Q-RT-PCR in FaDu/vehicle, and FaDu/Aurora-A transfectants treated with DMSO or GM6001 in a dose-dependent manner. Statistical analysis: **p < 0.01, ***p < 0.001.

    Mol Cancer, 2015, 14(1):83.. Ilomastat (GM6001, Galardin) purchased from Selleck.

  • ARPE-19 cells were seeded on Millicell inserts for growth to form the monolayer. Monolayers were treated with or without recombinant HIV-1 gp120 glycoprotein during the last 2 days of cell culture. Some samples were pretreated with anti-DC-SIGN antibodies or GM6001 before incubation with gp120. A, the TEER value was measured. B, the paracellular permeability for FITC-dextran flux was assessed. Date represent mean ± S.D. *, p < 0.05; **, p < 0.01; ***, p < 0.001. Ω, ohm.

    J Biol Chem, 2016, 291(44):22977-22987. Ilomastat (GM6001, Galardin) purchased from Selleck.

  • Immunofluorescence images of MMP-2 and MMP-9 in the ischemic brain 1 h after probe injection confirmed the sensitivity of the MMP-P12 probe in quantifying reduced MMP activity in response to MMP-specific inhibitors on day 7 post stroke (n = 5 per group).

    Sci Rep, 2015, 5:16951. Ilomastat (GM6001, Galardin) purchased from Selleck.

  • Immunoblotting of whole cell lysates obtained from phLFs treated with 1 ng/ml TGF-1 together with specific inhibitor targeting matrix metalloproteinases (MMPs; GM6001) every 24 h for a total 48-h treatment period. Cell lysates were probed for CDCP1, α-SMA and βactin. β-actin was used as a loading control. Untreated samples are indicated by “wo.” Each blot is representative of 3 independent experiments

    Am J Physiol Lung Cell Mol Physiol, 2018, 314(5):L695-L707. Ilomastat (GM6001, Galardin) purchased from Selleck.

  • Effect of the broad spectrum hydroxamate inhibitors batimastat and ilomastat on a disintegrin and metalloproteinase with thombospondin type 1 motifs (ADAMTS) 13 and ADAMTS15. (A) While batimastat is a good inhibitor against ADAMTS15, ilomastat has no ability to inhibit the enzyme. ADAMTS15 (20 nM) was pre-incubated with two doses (300 nM or 3 µM) of batimastat and ilomastat prior to the addition of aggrecan substrate G1-IGD-G2. The inhibitory effect of batimastat can be clearly discerned from the undigested 130 kDa G1-IGD-G2 bands.

    Biomed Rep, 2016, 4(1):73-78. . Ilomastat (GM6001, Galardin) purchased from Selleck.

Purity & Quality Control

Choose Selective MMP Inhibitors

Biological Activity

Description Ilomastat (GM6001, Galardin) 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)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEk293 cells NVTsd29TTnWwY4Tpc44h[XO|YYm= M2PzWmlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiQVTBUXRUPCCneIDy[ZN{\WRiaX6gTGVsOjl|IHPlcIx{KHW|aX7nJGZCVS2DRYfMVWdTWEmVSVHLMXRCVVKDIHHzJJN2[nO2cnH0[UBu\WG|dYLl[EBnd3JiMUWgcYlveyCkeTDmcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUC9NE41QCEQvF2= Mo\ENlM{PzZ7OUe=
human U251 cells NWjpVodbTnWwY4Tpc44h[XO|YYm= MVOyNEDPxE1? MXrQdo91\WO2aX;uJIFo[Wmwc4SgZY51cHKjeDDQRVY{NWyndHjhcEB1d3irbjDjc41xdGW6LXnu[JVk\WRiY4n0c5RwgGmlaYT5JIlvKGi3bXHuJHUzPTFiY3XscJMh[XRiMkCgeW0h[XRiNECwJI5oN22uIHL5JG1VXCC2ZYP0 NXzOe3hMOTd3M{e3NlE>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
MyoD / Myf5 / Myf6 / M-Cadherin / Notch1; 

PubMed: 23329998     


Gene expression was examined for 4 genes related to myogenic differentiation (MyoD, Myf5, Myf6 and M-cadherin) and 1 signaling gene (Notch1) after 3 and 6 hours pretreatment with GM6001 and 1 day cultured with myogenic differentiation meda. GAPDH was used䲧疝Ỵ疞㧀疜膉痘 

CD34 / Sca1; 

PubMed: 23329998     


The gene expression of MDSCs treated with 25μM of GM6001 for 3 and 6 hours. These results indicate that MDSCs treated with an MMP inhibitor had reduced expression of stem cell markers, CD34 and Sca1. GAPDH was used as a loading control.

23329998
Immunofluorescence
ZO-1 / Claudin-5 / occludin; 

PubMed: 21857898     


(A) Confocal imaging of ZO-1, claudin-5 and occludin of human BMEVCs; (B, C, D) BMEVCs co-cultured with SHI-1, HL-60 and U937 cells with or without treatment by GM6001. (E) BMEVCs of co-cultured with SHI-1 cells after knock-down of the MMP-2/MMP-9 gene. D䲧疝Ỵ疞㧀疜膉痘 瘿삨ՂᾰƌՂĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ՂĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸

21857898
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

Animal Research:

[4]

+ Expand
  • Animal Models: Rabbit
  • Formulation: 50 mM HEPES buffer
  • Dosages: 100 mg/kg/day
  • Administration: subcutaneous
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (200.79 mM)
Ethanol 8 mg/mL warmed (20.59 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
11mg/mL

* 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.

Chemical Information

Molecular Weight 388.46
Formula

C20H28N4O4

CAS No. 142880-36-2
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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MMP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID