GM 6001
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GM 6001 is a broad-spectrum inhibitor of MMP with Ki values of 0.4nM, 0.5nM, 27nM, 0.1nM and 0.2nM, respectively for MMP-1,2,3,8 and 9 [1].
MMPs are divided into 4 subfamilies: stromelysins, gelatinases, membrane-type MMPs, and collagenases. They play major roles in mediating the effects of IL-1 during meniscal healing. As an inhibitor of MMP, GM 6001 is reported to enhance the repair of meniscal lesions in an inflammatory microenvironment. MMPs also play roles in the transactivation of EGFR induced by GPCR agonists. It is reported that treatment of GM 6001 inhibits the phosphorylation of EGFR as well as the activation of ERK induced by bombesin or LPA. The DNA synthesis induced by bombesin or LPA is also attenuated by GM 6001 since the activity of MMP is required for the GPCR-induced late response mitogenic signaling [1, 2].
References:
[1] McNulty AL, Weinberg JB, Guilak F. Inhibition of matrix metalloproteinases enhances in vitro repair of the meniscus. Clin Orthop Relat Res. 2009 Jun;467(6):1557-67.
[2] Santiskulvong C, Rozengurt E. 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.
2. Lertudomphonwanit C, Mourya R, et al. "Large-scale proteomics identifies MMP-7 as a sentinel of epithelial injury and of biliary atresia." Sci Transl Med. 2017 Nov 22;9(417). PMID:29167395
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 388.46 |
| Cas No. | 142880-36-2 |
| Formula | C20H28N4O4 |
| Solubility | ≥19.423 mg/mL in DMSO, <2.47 mg/mL in EtOH, <2.43 mg/mL in H2O |
| Chemical Name | (2R)-N'-hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl]-2-(2-methylpropyl)butanediamide |
| SDF | Download SDF |
| Canonical SMILES | CC(C)CC(CC(=O)NO)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
| Cell experiment [1]: | |
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Cell lines |
MDA-MB-435 cells |
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Preparation method |
Soluble in DMSO > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
1, 2, 4 nM; 6 or 12 h. |
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Applications |
In MDA-MB-435 cells, GM 6001 increases the respiratory rate by 80% and [3H] thymidine incorporation by 50% when treated for 6 h and 12 h respectively, which suggest that GM 6001 increase DNA synthesis. GM 6001 also increases ERK activity and p38 kinase activity. |
| Animal experiment [2]: | |
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Animal models |
Rats with balloon injury of the carotid artery. |
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Dosage form |
100 mg/kg; 2, 4, 7, 10, or 14 days; IP injection. |
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Preparation method |
Dissolved in 4% CMC. |
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Applications |
GM 6001 reduces the amount of SMCs that migrated into the intima by 97% at 4 days after injury and inhibits lesions growth, which is mediated by MMP. However, at 14 days after injury, intimal area and the amount of SMCs were the same in GM 6001-treated and control rats. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Porter JF, Shen S, Denhardt DT. Tissue inhibitor of metalloproteinase-1 stimulates proliferation of human cancer cells by inhibiting a metalloproteinase. Br J Cancer, 2004, 90(2): 463-470. [2]. Bendeck MP, Irvin C, Reidy MA. Inhibition of matrix metalloproteinase activity inhibits smooth muscle cell migration but not neointimal thickening after arterial injury. Circ Res, 1996, 78(1): 38-43. | |
| Description | GM 6001 is a broad-spectrum inhibitor of MMP with Ki values of 0.4nM, 0.5nM, 27nM, 0.1nM and 0.2nM, for MMP-1,2,3,8 and 9, respectively. | |||||
| Targets | MMP-1 | MMP-2 | MMP-3 | MMP-8 | MMP-9 | |
| IC50 | 0.4 nM (Ki) | 0.5 nM (Ki) | 27 nM (Ki) | 0.1 nM (Ki) | 0.2 nM (Ki) | |
Quality Control & MSDS
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Chemical structure
Related Biological Data
Related Biological Data
