1. Metabolic Enzyme/Protease
  2. MMP

GM6001 (Synonyms: Galardin; Ilomastat; GM 6001; GM-6001)

Cat. No.: HY-15768 Purity: 98.23%
Data Sheet SDS Handling Instructions

GM6001 is a broad spectrum matrix metalloprotease (MMP) inhibitor, 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 for MMP-1/2/3/7/8/9/12/14/26, respectively.

For research use only. We do not sell to patients.
GM6001 Chemical Structure

GM6001 Chemical Structure

CAS No. : 142880-36-2

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10 mM * 1 mL in DMSO $99 In-stock
5 mg $90 In-stock
10 mg $150 In-stock
50 mg $450 In-stock
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Description

GM6001 is a broad spectrum matrix metalloprotease (MMP) inhibitor, 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 for MMP-1/2/3/7/8/9/12/14/26, respectively.

IC50 & Target

Ki: 0.4 nM (MMP-1), 0.5 nM (MMP-2), 27 nM (MMP-3), 3.7 nM (MMP-7), 0.1 nM (MMP-8), 0.2 nM (MMP-9), 3.6 nM (MMP-12), 13.4 nM (MMP-14), 0.36 nM (MMP-26)

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, and thus inhibits T-cell homing[4]

In Vivo

GM6001 (400 μg/mL) prevents corneal ulceration after severe alkali injury[2]. GM6001 significantly inhibits intimal hyperplasia and intimalcollagen content, and it increases lumen area in stented arteries without effects on proliferation rates in rabbit model after stenting[3].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.5743 mL 12.8713 mL 25.7427 mL
5 mM 0.5149 mL 2.5743 mL 5.1485 mL
10 mM 0.2574 mL 1.2871 mL 2.5743 mL
Kinase Assay
[1]

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.

Animal Administration
[3]

GM6001 is prepared in placebo.

To assess the effects of MMP inhibition, animals are given daily injections of either vehicle (“placebo group”) or GM6001 (100 mg/kg per day as subcutaneous suspension), beginning one day before the second injury until seven days after the procedure. GM6001 is a nonspecific hydroxamic acid-based MMPI with potent inhibitory activity against collagenase, gelatinases and stromelysin. Animals are euthanized at either 1 week or 10 weeks after the second injury. For biochemical studies, iliac artery tissue is removed under general anesthetic, followed by a fatal intracardiac injection of thiopentol. For histomorphometric studies, iliac arteries are perfusion-fixed in 10% buffered formalin for 20 min at a perfusion pressure of 80 mm Hg.

References
M.Wt

388.46

Formula

C₂₀H₂₈N₄O₄

CAS No.

142880-36-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 47 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.23%

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GM6001
Cat. No.:
HY-15768
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