Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
Products are for research use only. Not for human use. We do not sell to patients.
(Galardin; Ilomastat; GM 6001; GM-6001)
GM6001 Chemical Structure
|Product name: GM6001|
|Cat. No.: HY-15768|
GM6001 (galardin, ilomastat) is a broad spectrum MMPs inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki of 0.4-27 nM.
IC50 Value: 0.4-27 nM (Ki) 
in vitro: GM6001 (galardin, ilomastat) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 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, respectively. GM 6001 is one of the most potent inhibitors of human skin fibroblast collagenase yet reported. GM 6001 has a Ki of 20 nM against thermolysin and Pseudomonas aeruginosa elastase. Isomer 6B has a Ki of 7 nM against thermolysin and 2 nM against the elastase . Addition of galardin to cells stimulated with bombesin or LPA specifically inhibited total EGFR phosphorylation, as well as site-specific phosphorylation of tyrosine 845, a putative Src phosphorylation site, and tyrosine 1068, a typical autophosphorylation site. Galardin treatment also inhibited extracellular signal-regulated kinase (ERK) activation induced by bombesin or LPA, but not by EGF. In addition, galardin inhibited bombesin- or LPA-induced DNA synthesis in a dose dependent manner, when stimulated by increasing concentrations of bombesin, and when added after bombesin stimulation .
in vivo: Four full-thickness excisional wounds (50 mm2) on the back of 22 young female Sprague-Dawley rats, 12 treated with GM 6001 100 mg/kg and 10 with vehicle, were allowed to heal by secondary intention. GM 6001-treated wounds were minimally resurfaced with neoepithelium, despite unaltered keratinocyte proliferation in wound edges, whereas control wounds were completely covered with 3-7 cell layers of parakeratinized epithelium on post-wounding day 7 . Topical treatment of corneas with severe alkali injuries with 400 micrograms/ml or 40 micrograms/ml GM6001 alone prevented ulceration for 28 days, although 8 of 10 corneas treated with vehicle perforated. Corneas treated with 4 micrograms/ml GM6001 had midstromal depth ulcers. Corneas treated with 400 micrograms/ml of GM6001 contained very few inflammatory cells and had significantly reduced vessel ingrowth compared with vehicle-treated corneas .
|M.Wt||388.46||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: ≥ 47 mg/mL
|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|
. Santiskulvong C, et al. Galardin (GM 6001), a broad-spectrum matrix metalloproteinase inhibitor, blocks bombesin- and LPA-induced EGF receptor transactivation and DNA synthesis in rat-1 cells. Exp Cell Res. 2003 Nov 1;290(2):437-46.
. Mirastschijski U, et al. Matrix metalloproteinase inhibitor GM 6001 attenuates keratinocyte migration, contraction and myofibroblast formation in skin wounds. Exp Cell Res. 2004 Oct 1;299(2):465-75.
Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
CL-82198 is a selective inhibitor of MMP-13.
CTS-1027 is a potent small molecule inhibitor of MMPs(IC50=0.4 nM/0.6 nM for MMP2/MMP13); >1,000 fold selectivity over MMP1.
Edaravone(MCI-186), a strong novel free radical scavenger, is used for treatment of patients with acute brain infarction.
Isoginkgetin is a MMP-9 inhibitor, also a Pre-mRNA Splicing Inhibitor with IC 50 of 30 uM.
Marimastat(BB 2516; TA2516) is a broad spectrum inhibitor of MMPs (IC50 values are 3, 5, 6, 9 and 13 nM for MMP-9, MMP-1, MMP-2, MMP-14 and MMP-7 respectively).
NSC-405020 is a novel small molecule inhibitor of MT1-MMP that specifically targets PEX domain rather than the catalytic domain of MT1-MMP with IC50 >100 (mu)M and does not inhibit the catalytic activity of MT1-MMP or MMP-2.
SB-3CT is an effective and selective gelatinase inhibitor with Ki of 13.9 nM and 600 nM for MMP-2 and MMP-9, respectively.
TAPI-1 is a specific TACE(TNF-(alpha)-converting enzyme) inhibitor.
TAPI-2 is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factor(alpha)-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20(plusmn)10 (mu)M for MMP.
Other Countries & RegionsSee Worldwide Distributors