GM-6001


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

Description

Cas:142880-36-2

Product Information

GM-6001 is a broad-spectrum matrix metalloproteinase inhibitor with potential anticancer activity. GM6001 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.

 

Chemical Formula: C20H28N4O4

 

Exact Mass: 388.21106

 

Molecular Weight: 388.46072

 

Elemental Analysis: C, 61.84; H, 7.27; N, 14.42; O, 16.47

 

Synonym:

 

GM6001

GM-6001

GM 6001

Ilomastat

galardin

 

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

 

InChi Key: 

NITYDPDXAAFEIT-DYVFJYSZSA-N

 

InChi Code: 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

 

Smiles Code:

O=C(NC)[C@@H](NC([C@@H](CC(NO)=O)CC(C)C)=O)CC1=CNC2=CC=CC=C21

 

 

Technical Data:

 

Appearance: Beige to brown solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro:

Ilomastat (GM6001) inhibits human skin fibroblast collagenase, thermolysin and elastase with Kis of 0.4 nM, 20 nM, 20 nM, resepctively[1]. Ilomastat (0.1-10 nM) inhibits gelatinase A and gelatinase B produced by T-cells. Ilomastat inhibits T-cell homing.

 

In Vivo:

Ilomastat (GM6001) (400 μg/mL) inhibits corneal ulceration after severe alkali injury in animals. Ilomastat (GM6001) significantly suppresses intimal hyperplasia and intimalcollagen content. Ilomastat increases lumen area in stented arteries, shows no activity on proliferation rates in rabbit model after stenting.

References

 

  1. Bencsik P, Pálóczi J, Kocsis GF, Pipis J, Belecz I, Varga ZV, Csonka C, Görbe A, Csont T, Ferdinandy P. Moderate inhibition of myocardial matrix metalloproteinase-2 by ilomastat is cardioprotective. Pharmacol Res. 2014 Feb;80:36-42. doi: 10.1016/j.phrs.2013.12.007. Epub 2013 Dec 28. PubMed PMID: 24380772.

 

  1. Parkinson G, Gaisford S, Ru Q, Lockwood A, Khalili A, Sheridan R, Khaw PT, Brocchini S, Fadda HM. Characterisation of ilomastat for prolonged ocular drug release. AAPS PharmSciTech. 2012 Dec;13(4):1063-72. doi: 10.1208/s12249-012-9832-1. Epub 2012 Aug 18. PubMed PMID: 22903888; PubMed Central PMCID: PMC3513442.

 

  1. Senhao L, Dongqin Q. Preparation and in vitro evaluation of an ilomastat microemulsion gel by a self-microemulsifying system. Pharmazie. 2012 Feb;67(2):156-60. PubMed PMID: 22512086.

 

  1. Yeh DY, Lin HI, Feng NH, Chen CF, Wang D, Wang NT. Matrix metalloprotease expressions in both reperfusion lung injury and oleic acid lung injury models and the protective effects of ilomastat. Transplant Proc. 2009 Jun;41(5):1508-11. doi: 10.1016/j.transproceed.2009.02.076. PubMed PMID: 19545667.

 

  1. Wang YD, Wang W. Protective effect of ilomastat on trinitrobenzenesulfonic acid-induced ulcerative colitis in rats. World J Gastroenterol. 2008 Oct 7;14(37):5683-8. PubMed PMID: 18837084; PubMed Central PMCID: PMC2748202.

 

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

Payment & Security

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed