mmp-2/mmp-9 inhibitor i

MMP-2 MMP-9-IN-1 是一种有效的、具有高选择性和可口服的 IV 型胶原酶 (MMP-9和MMP-2) 抑制剂，对 MMP-9 和 MMP-2具有抑制作用， IC50分别为 0.24 和 0.3 1μM。MMP-2 MMP-9-IN-1 在肿瘤生长和转移的动物模型中展现出口服活性，可用于研究癌症。

BPHA (MMP-2 MMP-9 Inhibitor II) 是一种有效的、具有选择性和口服活性的抑制剂，对MMP-2、MMP-9 和 MMP-14 具有抑制作用，IC50 分别为 12 nM、16 nM 和 17 nM。BPHA 不抑制 MMP-1、-3 和 -7 (IC50 分别为 974、>1000 和 795 nM)。BPHA 具有抗血管生成和抗肿瘤活性。

MMP-9 inhibitor I is an inhibitor of matrix metalloproteinase-9 (MMP-9) that is selective over MMP-1 and MMP-13 (IC50s = 5, 1,050, and 113 nM, respectively). It also decreases the activity of TNF-α converting enzyme (TACE) in a dose-dependent manner (IC50 = 0.54 μM). MMP-9 inhibitor I decreases TNF-α secretion stimulated by LPS in BV-2 microglial cells when used at concentrations of 50 and 100 μM.

(R)-ND-336 is a highly potent and selective MMP-9 inhibitor, displaying a K i value of 19 nM. It also exhibits inhibitory activity against MMP-2 (K i = 127 nM) and MMP-14 (K i =119 nM). With its significant potential, (R)-ND-336 is being investigated in the field of diabetic foot ulcers (DFUs) research [1].