mmp-3 inhibitor

MMP-3 Inhibitor 是一种多肽基质金属蛋白酶-3（MMP-3）抑制剂，Ki 值为 95 nM。MMP-3 inhibitor 具有抗癌抗肿瘤活性。

MMP-3 Inhibitor acetate 是一种细胞渗透性强的人 MMP-3 抑制剂.

Matrix metalloproteinase-3 (MMP-3), also known as stromelysin-1, is a critical enzyme involved in tissue remodeling and repair through its role in degrading extracellular matrix proteins, facilitating cell migration. This enzyme has been implicated in various physiological processes including vascular remodeling associated with aneurysm formation, wound healing, the progression of atherosclerosis, and tumor initiation. MMP-3 inhibitor VIII, a cell-permeable sulfonamide-based hydroxamic acid, effectively inhibits MMP-3 by binding to its active site (Ki = 23 nM), thus blocking its enzymatic activity. Additionally, this inhibitor has been demonstrated to suppress the activity of mouse macrophage metalloelastase MME MMP-12, with an IC50 value of 13 nM, highlighting its potential utility in research on tissue remodeling and disease processes involving MMPs.

MMP3 inhibitor 1 is a potent and highly selective inhibitor of MMP-3 (IC50 of 1 nM).

MMP3 inhibitor 3 (TFA) 是一种MMP3的抑制剂，用于乳腺癌研究。

Ilomastat (GM6001) 是广谱的基质金属蛋白酶 (MMP) 抑制剂，可抑制 MMP 的活性，IC50值分别为 1.5 nM (MMP-1)，1.1 nM (MMP-2)，1.9 nM (MMP-3)，0.5 nM (MMP-9)，对人皮肤成纤维细胞胶原酶 (MMP-1) 的Ki=为 0.4 nM。

Marimastat (BB2516) 是一种血管生成和转移抑制剂，限制血管的生长和生成。它是一种广谱的，具有口服活性的MMPs 抑制剂，有效抑制 MMP-9 , MMP-1, MMP-2, MMP-14, MMP-7，用于癌症的研究。

Glucosamine sulfate (D-Glucosaminesulfate) 是软骨基质和滑液中糖胺聚糖的天然成分，常用作骨关节炎的治疗方法。它也是一种氨基糖，是糖基化蛋白和脂质生化合成的突出前体，用作膳食补充剂。

Muscone (3-Methylcyclopentadecanone) 是中药麝香的一种主要活性单体。它抑制NF-κB 和NLRP3炎性小体的活化，显著降低炎性细胞因子水平，并最终改善心脏功能和存活率。

Cordycepin (3'-Deoxyadenosine) 是一种核苷衍生物，在类风湿性关节炎滑膜成纤维细胞中，剂量依赖性抑制 IL-1β 诱导的 MMP-1和 MMP-3表达。它也抑制细菌的腺苷激酶从而抗结核分枝杆菌。

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8 9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26 DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630 624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20 2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

Batimastat (BB94) 是广谱MMP 抑制剂，能够抑制MMP-1 (IC50:3 nM)，MMP-2 (IC50:4 nM)，MMP-9 (IC50:4 nM)，MMP-7 (IC50:6 nM) 和 MMP-3 (IC50:20 nM)。

PD-166793是一种具有口服活性、有效性和选择性的 MMP 抑制剂，对 MMP-2，MMP-3 和 MMP-13 具有抑制作用。PD-166793 在大鼠心力衰竭模型中改善心肌缺血和再灌注损伤。

MMP2-IN-3是一种有效的基质金属蛋白酶（MMP-2）抑制剂（ IC50 值：31 μM）。MMP2-IN-3 抑制 MMP-9 和 MMP-8 ，其 IC50 分别为 26.6 和 32 μM。

Batimastat (BB-94) sodium salt is a broad-spectrum MMP inhibitor (IC50s: 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7, and MMP-3).

Prinomastat hydrochloride is a orally active inhibitor of metalloproteinase (MMP)(MMP-1, MMP-3 and MMP-9 with IC50s of 79, 6.3 and 5.0 nM , respectively),with Antitumor avtivity.

Prinomastat (AG3340) 是一种可穿过血脑屏障且具有口服活性和选择性的金属蛋白酶 (MMP) 抑制剂，抗肿瘤活性，对金属蛋白酶具有广谱的抑制作用，对 MMP-1, MMP-3 和 MMP-9 的抑制作用较强。

UK-370106 is a potent and highly selective inhibitor of MMP-3 with IC50 of 23 nM and MMP-12 with IC50 of 42 nM, and potently inhibits cleavage of [3H]-fibronectin by MMP-3 (IC50: 320 nM).

XL-784 free base is a selective inhibitor of matrix metalloproteinases (MMP), (IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13,respectively).

XL-784 is a selective inhibitor of matrix metalloproteinases (MMP)(IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13,respectively).

Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces and a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM, it also is an apoptosis inducer. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase, it also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin has antiproliferative and antitumor activities[1][2][3][4][5].

ARP-100 (MMP-2 Inhibitor III) 是选择性基质金属蛋白酶MMP-2抑制剂 (IC50=12 nM)。它对 MMP-1 (>50 μM)，MMP-3 (4.5 μM)，MMP-7 (>50 μM) 和MMP-9 (0.2 μM) 的抑制活性较小。它与 MMP-2 的 S1＇口袋相互作用，并在体外对基质胶的侵袭模型中显示抗侵袭特性。

经化学修饰的四环素 （CMTs） 可抑制 MMPs，但缺乏抗菌活性。四环素的非抗菌衍生物称为 incyclinide (COL-3, CMT-3)。 实验证明，Incyclinide（CMT-3） 可抑制前列腺癌、结肠腺癌和黑色素瘤在细胞培养中的侵袭性，并抑制肿瘤的生长和转移。

MMP13-IN-3 是口服有效的MMP-13选择性抑制剂，IC50为 1 nM，比其他 MMP 的选择性高 1000倍多。MMP13-IN-3在用于骨关节炎方面有研究的价值。