Ilomastat (GM6001, Galardin)

Catalog No.S7157

For research use only.

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.

Ilomastat (GM6001, Galardin) Chemical Structure

CAS No. 142880-36-2

Selleck's Ilomastat (GM6001, Galardin) has been cited by 41 publications

Purity & Quality Control

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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)
Click to View More Targets
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 MYHGeY5kfGmxbjDhd5NigQ>? Ml3PTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCDRFHNWHM1KGW6cILld5Nm\CCrbjDISYszQTNiY3XscJMhfXOrbnegSmFONUGHd1zRS3JRUVOLQVutWGFOWkFiYYOgd5Vje3S{YYTlJI1m[XO3cnXkJIZweiBzNTDtbY5{KGK7IH\seY9zd22ndILpZ{BidmGueYPpd{whUUN3ME2wMlQ5KM7:TR?= NETycHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3Olk6Pyd-MkOzO|Y6QTd:L3G+
U251 cells M2Xw[GZ2dmO2aX;uJIF{e2G7 MY[yNEDPxE1? MmP6VJJwfGWldHnvckBi\2GrboP0JIFvfGi{YYigVGE3Oy2uZYToZYwhfG:6aX6gZ49ueGyneD3pcoR2[2WmIHP5eI91d3irY3n0fUBqdiCqdX3hckBWOjVzIHPlcIx{KGG2IEKwJJVOKGG2IESwNEBv\y:vbDDifUBOXFRidHXzeC=> MkHTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3M{e3NlEoRjF5NUO3O|IyRC:jPh?=
HEk293 cells M3O2S2Z2dmO2aX;uJIF{e2G7 M2nlNWlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiQVTBUXRUPSCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KHW|aX7nJGFjgi2WRWPFe3NTT0GLWT3EdIEuU0tiYYOgd5Vje3S{YYTlJI1m[XO3cnXkJIZweiB{IHjyd{BjgSCobIXvdo9u\XS{aXOgZY5idHm|aYOsJGlEPTB;MD61JO69VQ>? Mn\5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{[5PVcoRjJ|M{e2PVk4RC:jPh?=
Assay
Methods Test Index PMID
Western blot MyoD / Myf5 / Myf6 / M-Cadherin / Notch1 ; CD34 / Sca1 23329998
Immunofluorescence ZO-1 / Claudin-5 / occludin 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 (from reference)

Animal Research:

[4]

  • Animal Models: Rabbit
  • Dosages: 100 mg/kg/day
  • Administration: subcutaneous

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

Chemical Information

Molecular Weight 388.46
Formula

C20H28N4O4

CAS No. 142880-36-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)CC(CC(=O)NO)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

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.

Handling Instructions

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