Marimastat (BB2516) (BB-2516) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor. MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM)and MMP-7 (IC50=13 nM).

MMP14:9 nM, MMP9:3 nM, MMP7:13 nM, MMP2:6 nM, MMP1:5 nM

Marimastat (BB-2516) 是一种具有广谱MMPI活性的化合物，其酶抑制谱与batimastat非常相似。Marimastat以1μM(IC50)抑制Karpas 299细胞中CD30的脱落，并且以剂量依赖的方式抑制LPS诱导的可溶性TNF-α产生。与基质金属蛋白酶紧密相关的酶，肿瘤坏死因子α转换酶(TACE)，负责将前体TNFα处理成TNFα，Marimastat特异性地以3.8纳摩(IC50)抑制该酶。

Marimastat在人体中具有良好的药代动力学特性，口服给药后几乎完全吸收，具有高且可预测的生物利用度，半衰期约为15小时（说明每天两次给药是可行的），使其成为临床试验中比batimastat更受欢迎的治疗选择。Marimastat在啮齿动物体内迅速代谢，经历极高的首过效应，这使得在啮齿动物中测试Marimastat变得困难，因为在这种物种中难以获得持续的血浆浓度。[1]

Compounds 1, 2, 7-9 and 11-16 are pre-incubated with MMP-1 or MMP-3 (10 nM) at different concentrations (0-10 μM) in a mixture of Tris-HCl (50 mM, pH 7.5), NaCl (150 mM), CaCl2 (10 mM), NaN3 (0.02%) and Brij-35 (0.05%) for 1 hour at 37°C. Residual activity is measured using the fluorogenic MMP substrate (2 μM) by fluorescence increase (emission at 393 nm and excitation at 325 nm) on a fluorescence plate reader. The data are fitted to the tight binding inhibitor equation: v=[(E-I-k+[(E-I-k)2+4Ek]1/2)/(2E)], where v is the velocity of the reaction, E is the enzyme concentration, I is the initial inhibitor concentration, and k is the apparent inhibition constant, using the software Prism.