For research use only. Not for therapeutic Use.
Ilomastat, also known as GM6001 or Galardin, is a potent inhibitor of matrix metalloproteases (MMPs) that exhibits broad-spectrum activity. It can effectively inhibit the activity of several MMPs, including MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26, with Ki values ranging from 0.1 nM to 27 nM. Specifically, the Ki values for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 are 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 13.4 nM, and 3.6 nM, respectively. Additionally, Ilomastat has a Ki value of 0.36 nM for MMP-13.
| Catalog Number | I001644 |
| CAS Number | 142880-36-2 |
| Synonyms | (2R)-N/’-hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl]-2-(2-methylpropyl)butanediamide |
| Molecular Formula | C₂₀H₂₈N₄O₄ |
| Purity | ≥95% |
| Target | MMP |
| Solubility | DMSO: ≥ 47 mg/mL |
| Storage | 2-8°C |
| IC50 | 0.4-27 nM (Ki) |
| IUPAC Name | (2R)-N'-hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl]-2-(2-methylpropyl)butanediamide |
| 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 |
| InChIKey | NITYDPDXAAFEIT-DYVFJYSZSA-N |
| SMILES | CC(C)CC(CC(=O)NO)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC |
| Reference | </br>1:GM6001 Increases Anastomotic Leakage following Colonic Obstruction Possibly by Impeding Epithelialization. Rehn M, Krarup PM, Christensen LH, Seidelin JB, Ågren MS, Syk I.Surg Infect (Larchmt). 2015 Dec;16(6):702-8. doi: 10.1089/sur.2014.248. Epub 2015 Jul 14. PMID: 26171681 Free PMC Article</br>2:Efficacy of GM6001 as an adjuvant to ceftriaxone in a neonatal rat model of Streptococcus pneumoniae meningitis. Liu X, Han Q.Acta Neurobiol Exp (Wars). 2014;74(4):489-96. PMID: 25576979 Free Article</br>3:[GM6001 suppresses scar formation after glaucoma filtration surgery in rabbits]. Shen Y, Wu W, Lu X, Guo W.Nan Fang Yi Ke Da Xue Xue Bao. 2014 Feb;34(2):241-5. Chinese. PMID: 24589605 Free Article</br>4:Monocyte-derived dendritic cell subpopulations use different types of matrix metalloproteinases inhibited by GM6001. Kis-Toth K, Bacskai I, Gogolak P, Mazlo A, Szatmari I, Rajnavolgyi E.Immunobiology. 2013 Nov;218(11):1361-9. doi: 10.1016/j.imbio.2013.06.012. Epub 2013 Jul 2. PMID: 23870824 </br>5:[Effects of matrix metalloproteinases inhibitor GM6001 on choroidal neovascularization]. Chen XG, He SZ.Zhonghua Yan Ke Za Zhi. 2012 Aug;48(8):744-9. Chinese. PMID: 23141517 </br>6:The effect of MMP inhibitor GM6001 on early fibroblast-mediated collagen matrix contraction is correlated to a decrease in cell protrusive activity. Martin-Martin B, Tovell V, Dahlmann-Noor AH, Khaw PT, Bailly M.Eur J Cell Biol. 2011 Jan;90(1):26-36. doi: 10.1016/j.ejcb.2010.09.008. Epub 2010 Nov 1. PMID: 21040999 </br>7:[Effect of GM6001 on the model that cervical squamous carcinoma cell line HCE1 multicellular spheroids invade live human umbilical vein endothelium cell monolayers]. Lan J, Wu Y.Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2010 Aug;35(8):868-74. doi: 10.3969/j.issn.1672-7347.2010.08.016. Chinese. PMID: 20818082 Free Article</br>8:Effects of the matrix metalloproteinase inhibitor GM6001 on the destruction and alteration of epithelial basement membrane during the healing of post-alkali burn in rabbit cornea. Kato T, Saika S, Ohnishi Y.Jpn J Ophthalmol. 2006 Mar-Apr;50(2):90-5. PMID: 16604381 </br>9:Metalloprotease inhibitors GM6001 and TAPI-0 inhibit the obligate intracellular human pathogen Chlamydia trachomatis by targeting peptide deformylase of the bacterium. Balakrishnan A, Patel B, Sieber SA, Chen D, Pachikara N, Zhong G, Cravatt BF, Fan H.J Biol Chem. 2006 Jun 16;281(24):16691-9. Epub 2006 Mar 24. PMID: 16565079 Free Article</br>10:Efficacy of albendazole-GM6001 co-therapy against Angiostrongylus cantonensis-induced meningitis in BALB/c mice. Lai SC, Jiang ST, Chen KM, Hsu JD, Shyu LY, Lee HH.Acta Trop. 2005 Mar;93(3):267-73. PMID: 15716044 |
