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]。