GM-6001


Catalog No. size PriceQuantity
M6410-2 2mg solid $134
M6410-10 10mg solid $534

Description

GM-6001 is a broad-spectrum matrix metalloproteinase inhibitor with potential anticancer activity. GM-6001 is a member of the hydroxamic acid class of reversible metallopeptidase inhibitors. The anionic state of the hydroxamic acid group forms a bidentate complex with the active site zinc. Examples of enzymes that ilomastat inhibit include thermolysin, peptide deformylase, and anthrax lethal factor endopeptidase (LF) produced by the bacterium Bacillus anthracis.

Product information

CAS Number: 142880-36-2

Molecular Weight: 388.46

Formula: C20H28N4O4

Synonym:

Ilomastat

galardin

Chemical Name:  (R)-N1-((S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl)-N4-hydroxy-2-isobutylsuccinamide

Smiles: CC(C)C[C@H](CC(=O)NO)C(=O)N[C@@H](CC1=CNC2=CC=CC=C12)C(=O)NC

InChiKey: NITYDPDXAAFEIT-DYVFJYSZSA-N

InChi: InChI=1S/C20H28N4O4/c1-12(2)8-13(10-18(25)24-28)19(26)23-17(20(27)21-3)9-14-11-22-16-7-5-4-6-15(14)16/h4-7,11-13,17,22,28H,8-10H2,1-3H3,(H,21,27)(H,23,26)(H,24,25)/t13-,17+/m1/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

GM-6001 inhibits human skin fibroblast collagenase, thermolysin and elastase with Kis of 0.4 nM, 20 nM, 20 nM, resepctively. GM-6001 (0.1-10 nM) inhibits gelatinase A and gelatinase B produced by T-cells. GM-6001 inhibits T-cell homing.

In Vivo:

GM-6001 (400 μg/mL) inhibits corneal ulceration after severe alkali injury in animals. GM-6001 significantly suppresses intimal hyperplasia and intimalcollagen content. GM-6001 increases lumen area in stented arteries, shows no activity on proliferation rates in rabbit model after stenting.

References:

  1. Grobelny D, et al. Inhibition of human skin fibroblast collagenase, thermolysin, and Pseudomonas aeruginosa elastase by peptide hydroxamic acids. Biochemistry. 1992 Aug 11;31(31):7152-4.
  2. Schultz GS, et al. Treatment of alkali-injured rabbit corneas with a synthetic inhibitor of matrix metalloproteinases. Invest Ophthalmol Vis Sci. 1992 Nov;33(12):3325-31.
  3. Li C, et al. Arterial repair after stenting and the effects of GM6001, a matrix metalloproteinase inhibitor. J Am Coll Cardiol. 2002 Jun 5;39(11):1852-8.
  4. Leppert D, et al. T cell gelatinases mediate basement membrane transmigration in vitro. J Immunol. 1995 May 1;154(9):4379-89.
  5. Yamamoto M, et al. Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket. J Med Chem. 1998 Apr 9;41(8):1209-17.

Products are for research use only. Not for human use.

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