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
Chemical Name: (R)-N1-((S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl)-N4-hydroxy-2-isobutylsuccinamide
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
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
Ilomastat (GM6001) inhibits human skin fibroblast collagenase, thermolysin and elastase with Kis of 0.4 nM, 20 nM, 20 nM, resepctively. Ilomastat (0.1-10 nM) inhibits gelatinase A and gelatinase B produced by T-cells. Ilomastat inhibits T-cell homing.
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.
Bencsik P, PÃ¡lÃ³czi J, Kocsis GF, Pipis J, Belecz I, Varga ZV, Csonka C, GÃ¶rbe 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.
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.
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.
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.
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.
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