GM 6001
(Synonyms: 伊洛马司他; GM6001; Galardin) 目录号 : GC14523
GM 6001 是一种广谱 MMP 抑制剂，可用于癌症和神经退行性疾病的研究，GM 6001对 MMP-1、2、3、8 和 9 的 Ki 值分别为 0.4、0.5、27、0.1和 0.2 nM。
Cas No.:142880-36-2
Sample solution is provided at 25 µL, 10mM.
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GM 6001 is a broad-spectrum MMP inhibitor that can be used in the study of cancer and neurodegenerative diseases. The Ki values of GM 6001 for MMP-1, 2, 3, 8 and 9 are 0.4, 0.5, 27, 0.1 and 0.2 nM, respectively[1-4].
GM 6001 (25 μM) can inhibit the decrease of E-cadherin expression and increase of vimentin expression induced by TGF-β1[2]. In addition, GM 6001 can also inhibit the proliferation and invasion of MDA-MB-231 cells and promote cell apoptosis[3].
GM 6001 (100 mg/kg) can significantly reduce pro-MMP-9 and active-MMP-9 levels in MPTP-induced Parkinson's disease mouse model[4]. GM 6001 (1.2mg/kg) treatment significantly reduced the mean blood pressure of Dahl/SS rats, inhibited the expression and activity of MMP-9 and significantly improved oxidative/nitrosative stress and TJPs, restoring Dahl/SS rats vascular integrity[5].
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] Bai X, Li YY, Zhang HY, Wang F, He HL, Yao JC, Liu L, Li SS. Role of matrix metalloproteinase-9 in transforming growth factor-β1-induced epithelial-mesenchymal transition in esophageal squamous cell carcinoma. Onco Targets Ther. 2017 Jun 2;10:2837-2847.
[3] Cui Q, Wang B, Li K, et al. Upregulating MMP-1 in carcinoma-associated fibroblasts reduces the efficacy of Taxotere on breast cancer synergized by Collagen IV[J]. Oncology letters, 2018, 16(3): 3537-3544.
[4] Si X, Dai S, Fang Y, et al. Matrix metalloproteinase-9 inhibition prevents aquaporin-4 depolarization-mediated glymphatic dysfunction in Parkinson’s disease[J]. Journal of advanced research, 2024, 56: 125-136.
[5] Kalani A, Pushpakumar S B, Vacek J C, et al. Inhibition of MMP-9 attenuates hypertensive cerebrovascular dysfunction in Dahl salt-sensitive rats[J]. Molecular and cellular biochemistry, 2016, 413: 25-35.
GM 6001 是一种广谱 MMP 抑制剂，可用于癌症和神经退行性疾病的研究，GM 6001对 MMP-1、2、3、8 和 9 的 Ki 值分别为 0.4、0.5、27、0.1和 0.2 nM [1-4]。
GM 6001 （25 μM）可以抑制 TGF-β1 诱导的 E-钙粘蛋白表达减少和波形蛋白表达增加[2]，并且，GM 6001也可以抑制MDA-MB-231细胞的增殖和侵袭，促进细胞凋亡[3]。
GM 6001 (100 mg/kg) 可以显著降低MPTP 诱导的帕金森疾病小鼠模型中pro-MMP-9 和 active-MMP-9 水平[4]。GM 6001 (1.2 mg/kg)治疗显著降低了 Dahl/SS 大鼠的平均血压，抑制MMP-9 的表达和活性，并且显着改善了氧化/亚硝化应激和 TJPs， 恢复Dahl/SS 大鼠血管完整性[5]。
| Cell experiment [1]: | |
Cell lines | Human OSCC cell line, SCC-15 |
Preparation Method | GM 6001 (100 μM) was added to the culture medium to culture the cells. Western blot was used to detect the expression of ephrinA1 protein at 24 h and 48 h. |
Reaction Conditions | 100μM, 24h and 48h |
Applications | GM 6001 can significantly reduce ephrinA1 protein in the supernatant of hypoxic cancer cells. |
| Animal experiment [2]: | |
Animal models | New steroid-induced necrosis of femoral head（SINFH） rats |
Preparation Method | A total of 120 rats were divided into four groups: 1. WT negative control group 2. WT+GM 6001 group 3. SINFH model positive control group 4. SINFH model + GM 6001 group. GM 6001 was injected into the tail vein once a week at 70 mg/kg for a total of 8 injections. |
Dosage form | 70 mg/kg, once a week, 8 weeks, i.v. |
Applications | Serum calcium and phosphorus levels, BGP levels, femoral head density, and osteoblast counts were all higher in the GM 6001 group than in the SINFH model group. |
References: | |
| Cas No. | 142880-36-2 | SDF | |
| 别名 | 伊洛马司他; GM6001; Galardin | ||
| 化学名 | (2R)-N'-hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl]-2-(2-methylpropyl)butanediamide | ||
| Canonical SMILES | CC(C)CC(CC(=O)NO)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC | ||
| 分子式 | C20H28N4O4 | 分子量 | 388.46 |
| 溶解度 | ≥ 19.423 mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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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 |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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2.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet