mmp-3 inhibitor 1

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

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。

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)。

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。

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。

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。

Broad spectrum MMP inhibitor (IC_{50< sub> values are 0.7, 0.9, 13, 16 and 1170 nM for MMP-2, MMP-13, MMP-9, MMP-3 and MMP-1 respectively). Attenuates early left ventricular dilation after experimental myocardial infarction in mice.}

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 inhibitor I is a peptide inhibitor of matrix metalloproteinase-1 (MMP-1), MMP-2, and MMP-3 (IC50s = 1.3, 30, and 150 μM, respectively). It is selective for MMP-1, MMP-2, and MMP-3 over the proteases thermolysin, urease, trypsin, α-chymotrypsin, plasmin, and elastase at concentrations up to 4 mM.

GM 1489 is a broad-spectrum inhibitor of matrix metalloproteinases (MMPs) with Ki values of 0.002, 0.1, 0.5, 0.2, and 20 μM for MMP-1, MMP-8, MMP-2, MMP-9, and MMP-3, respectively. It reduces 5-aza-2'-deoxycytidine-induced increases in MMP-1, MMP-2, MMP-3, MMP-7, MMP-9, and MMP-14 expression as well as cell invasion in AsPC-1, BxPC-3, Hs766T, MiaPaCa2, and PANC-1 cancer cells. Topical administration of GM 1489 (100 μg) inhibits increases in ear thickness and epidermal hyperplasia induced by phorbol 12-myristate 13-acetate and phorbol dibutyrate (PdiBu) in mice.

Luteolin 7-O-glucuronide (Luteolin-7-glucuronide) 是一种自由基清除剂，能够抑制基质金属蛋白酶的活性，其对 MMP-1，MMP-3，MMP-8，MMP-9，MMP-13的IC50值分别为 17.63，7.99，11.42，12.85，0.03 μM。

MMP13-IN-2 is a highly potent, selective, and orally active inhibitor of MMP-13. It demonstrates exceptional potency against MMP-13, with an IC50 value of 0.036 nM, and exhibits selectivities greater than 1,500-fold over MMP-1, 3, 7, 8, 9, 14, and TACE. Moreover, MMP13-IN-2 possesses the capability to effectively inhibit collagen release from cartilage in vitro. Consequently, MMP13-IN-2 holds great potential for advancing research on collagenase-related diseases.

T-5224 是选择性的转录因子c-Fos activator protein (AP)-1抑制剂，具有抗炎作用，能够特异性抑制 c-Fos c-Jun 的 DNA 结合活性，但对其他转录因子的结合活性无影响。它抑制 IL-1β 诱导的 Mmp-3、Mmp-13、Adamts-5 转录上调。

FAK-IN-3 是一种有效的粘着斑激酶 (FAK) 抑制剂。FAK-IN-3 能够减少 PA-1 细胞的迁移和侵袭，并抑制 MMP-2 和 MMP-9 的表达。FAK-IN-3 对肿瘤生长和转移具有抑制作用，且没有明显不良反应。FAK-IN-3 对卵巢癌表现出研究潜力。

AS1940477 is p38 MAPK inhibitor. AS1940477 inhibited the enzymatic activity of recombinant p38α and β isoforms but showed no effect against other 100 protein kinases including p38γ and δ isoforms. In human peripheral blood mononuclear cells, AS1940477 inhibited lipopolysaccharide (LPS)- or phytohemagglutinin A (PHA)-induced production of proinflammatory cytokines, including TNFα, IL-1β, and IL-6 at low concentrations (LPS TNFα, IC(50)=0.45n M; PHA TNFα, IC(50)=0.40 nM). In addition, equivalent concentrations of AS1940477 that inhibited cytokine production also inhibited TNFα- and IL-1 β-induced production of IL-6, PGE(2), and MMP-3 in human synovial stromal cells. AS1940477 was also found to potently inhibit TNF production in whole blood (IC(50)=12 nM) and effectively inhibited TNFα production induced by systemically administered LPS in rats at less than 0.1mg kg (ED(50)=0.053 mg kg) with an anti-inflammatory effect lasting for 20h after oral administration. Overall, this stu......

Doxycycline calcium 是一种具有口服活性的四环素类抗生素，同时作为广谱金属蛋白酶（MMP）抑制剂，具有抗菌和抗肿瘤细胞增殖活性，常用于诱导基因表达的 ON-OFF 体系。

MMP-9-IN-8（Compound 3）是MMP-9抑制剂，10 μM浓度下抑制活性为42.16%，50 μM时达58.28%。该化合物展现抗癌活性，能诱导MCF-7细胞凋亡，IC50为23.42 μM。