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(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
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