GM 6001
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
GM 6001(Ilomastat,Galardin)是一种广谱MMP抑制剂,作用于MMP-1、MMP-2、MMP-3、MMP-8和MMP-9,Ki值分别为0.4 nM、0.5 nM、27 nM、0.1 nM和0.2 nM [1]。
MMPs分为四个亚家族,分别是溶基质素(stromelysins),明胶酶(gelatinases),膜型基质金属蛋白酶(membrane-type MMPs)和胶原酶(collagenases)。MMPs在半月板修复中介导IL-1的作用。同时,MMPs在GPCR激动剂诱导的EGFR的转录激活中也起到重要作用。GM 6001可以增强炎症微环境下半月板损伤的修复。由于MMP活性对于GPCR诱导的延迟反应有丝分裂信号是必须的,GM 6001也可以减弱蛙皮素(bombesin)或LPA诱导的DNA的合成 [1, 2]。GM 6001处理可以抑制蛙皮素(bombesin)或LPA诱导的EGFR的磷酸化和ERK的激活。
参考文献:
[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.
- 1. Wenlong Zhang, Qing Zhang, et al. "Crosstalk between IL‐15Rα+ tumor‐associated macrophages and breast cancer cells reduces CD8+ T cell recruitment." Cancer Commun (Lond). 2022 Jun;42(6):536-557. PMID: 35615815
- 2. Mona Nazemi. "ECM internalisation as a novel modulator of cancer cell growth/survival." The University of Sheffield. April 2021.
- 3. Tan Ma, Yuan Zhou, et al. "Maternal exposure to di-n-butyl phthalate promotes the formation of testicular tight junctions through downregulation of NF-#B/COX-2/PGE2/MMP-2 in mouse offspring." Environ Sci Technol. 2020 Jul 7;54(13):8245-8258. PMID: 32525310
- 4. Tewari BP, Chaunsali L, et al. "Perineuronal nets decrease membrane capacitance of peritumoral fast spiking interneurons in a model of epilepsy." Nat Commun. 2018 Nov 9;9(1):4724. PMID: 30413686
- 5. 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 | insoluble in H2O; insoluble in EtOH; ≥19.42 mg/mL in DMSO |
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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
MDA-MB-435细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月 |
反应条件 |
1、2、4 nM,6或12 h. |
实验结果 |
在MDA-MB-435细胞中,GM 6001处理6小时和12小时后,呼吸速率增加80%,[3H]胸苷掺入增加50%,这表明GM 6001增加DNA合成。GM 6001还增加ERK活性和p38激酶活性。 |
动物实验 [2]: | |
动物模型 |
颈动脉气囊损伤大鼠 |
剂量 |
100 mg/kg,2、4、7、10或14天,腹腔注射。 |
溶解方法 |
溶于4% CMC. |
实验结果 |
损伤后第4天,GM 6001将迁移到内膜中的SMC的量减少97%,并抑制MMP介导的损伤生长。然而,在损伤后第14天,GM6001治疗组和对照大鼠中内膜区域和SMC的量相同。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
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. |
描述 | GM 6001(Ilomastat,Galardin)是一种广谱matrix metalloprotease (MMP)(基质金属蛋白酶)抑制剂,作用于MMP-1、MMP-2、MMP-3、MMP-8和MMP-9,Ki值分别为0.4 nM、0.5 nM、27 nM、0.1 nM和0.2 nM。 | |||||
靶点 | 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) |
质量控制和MSDS
- 批次:
化学结构
![GM 6001](http://www.apexbt.com//media/diy/images/struct/A4050.png)
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