mmp‐9

MMP-9-IN-7抑制前基质金属蛋白酶活化,可用于预防、治疗或改善 MMP9和/或 MMP13介导的综合征。

MMP-9-IN-6 是一种 MMP-9 抑制剂，其 IC50 值为50 μM, 具有较好的抗溃疡功效。MMP-9-IN-6 具有潜在的抗肿瘤活性，可用于研究组织重塑、伤口修复和动脉粥样硬化。

MMP-9-IN-1 是特异性的基质金属蛋白酶-9 抑制剂，选择性靶向 MMP-9 的血红素域，对其他 MMP 无影响。

MMP-9-IN-5 是一种 MMP-9 抑制剂，其 IC50 值为 4.49 nM，能够与 MMP-9 形成氢键。MMP-9-IN-5 也抑制 AKT 活性，其 IC50 值为 1.34 nM。MMP-9-IN-5 表现出细胞毒性，可诱导细胞凋亡 (apoptosis)，能够用于研究癌症。

MMP-9 MMP-13 Inhibitor I 是 MMP-9 和 MMP-13 双重抑制剂，IC50 均为 0.9 nM。MMP-9 MMP-13 Inhibitor I 对 MMP-9 MMP-13 的选择性是其他 MMP 的 20 倍以上。

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。

MMP-9-IN-4 是 MMP-9 抑制剂，能够与 MMP-9 形成 H-π 相互作用，IC50 值为 7.46 nM。MMP-9-IN-4 还能够抑制 AKT 活性，其 IC50 值为 8.82 nM。MMP-9-IN-4 能够诱导细胞凋亡 (apoptosis)，显示出细胞毒性，能够用于研究癌症。

MMP-9-IN-3 是一种 MMP-9 抑制剂 (IC50: 5.56 nM)，可与 MMP-9 形成氢键。MMP-9-IN-3 对 AKT 的活性具有抑制作用 (IC50: 2.11 nM)。MMP-9-IN-3 具有细胞毒性，能够诱导细胞凋亡。MMP-9-IN-3 能够用于研究癌症。

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。

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.

MMP-2 9-IN-1 (Compound 4a) 是一种有效的 MMP-2 (IC50: 56 nM) 和 MMP-9 (IC50: 38 nM) 双重抑制剂。MMP-2 9-IN-1 对肿瘤生长具有抑制作用，明显诱导癌细胞凋亡 (apoptosis)，抑制细胞迁移，并抑制细胞周期进程导致 DNA 片段化。

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。

Ethyl gallate (gallic acid ethyl ester) 是一种非类黄酮酚过氧化氢清除剂。

Norepinephrine (Levophed) 属于生物碱类天然产物，是一种神经递质，一种肾上腺素能受体 (AR) 的激动剂，对 α1、α2 和 β1 AR 具有激活活性。Norepinephrine 被用作抗休克的血管活性剂。

Astragaloside IV (AS-IV) 是从黄芪中分离得到的一种皂苷，抑制ERK1 2和JNK 激活，在乳腺癌细胞 MDA-MB-231 中，下调(MMP)-2和(MMP)-9的信号通路。

Edaravone (MCI-186) 是一种新型自由基清除剂，能够抑制大鼠与 MMP-9有关的脑出血。

Histatin 5 acetate 抑制宿主基质金属蛋白酶 MMP-2 和 MMP-9 的活性，IC50 分别为 0.57 和 0.25 μM。

CTTHWGFTLC, CYCLIC acetate(244082-19-7 free base) 是基质金属蛋白酶 (MMP)-2 和 MMP-9 的抑制剂。它也被称为IV 型胶原酶或明胶酶。明胶酶是癌症治疗干预的潜在靶点，这些酶的抑制剂可以防止肿瘤进展。

Rebimastat 是基于巯基的第二代基质金属蛋白酶(MMP)抑制剂，具有潜在的抗肿瘤活性。利莫司他选择性抑制几种 MMPs (MMP 1、2、8、9和14)，从而诱导细胞外基质降解，抑制血管生成、肿瘤生长、侵袭和转移。

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)。

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。

Hinokiflavone 是pre-mRNA 剪接活性的新型调节剂，通过抑制剪接体装配来阻止pre-mRNA 底物的剪接，特别是阻止 B complex 的形成。它是SUMO protease 蛋白酶抑制剂，能够抑制前哨蛋白特异性蛋白酶 1 的活性。

Arg-Gly-Asp-Ser is an integrin-binding sequence that inhibits integrin receptor function. It decreases systemic inflammation via inhibition of collagen-triggered activation of leukocytes and attenuates expression of inflammatory cytokines, MMP-9, and iNOS

Glycitein (Glycetein) 是一种大豆异黄酮，可研究抗氧化和细胞凋亡。

NFAT Inhibitor (VIVIT peptide) 是NFAT 的细胞渗透性肽抑制剂，能够选择性抑制钙调磷酸酶介导的NFAT 脱磷酸作用。

SB-3CT 是一种可透过血脑屏障的、竞争性的金属蛋白酶MMP-2和MMP-9抑制剂，Ki 分别为 13.9 nM、600 nM。他对明胶酶具有高选择性。它具有神经保护和抗癌作用。

Salvianolic acid A (Dan Phenolic Acid A) 属于天然产物，是一种基质金属钛酶 9 (MMP-9) 的抑制剂。Salvianolic acid A 具有抗氧化和抗炎活性，可以保护血脑屏障。

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.

6-Shogaol (6-Shogaol) 是从生姜中分离的一种天然产物，具有抗癌、抗炎和抗氧化的多种生物活性。

JNJ0966 是高选择性 MMP-9酶原抑制剂，其 IC50=440 nM。

Glaucine 是从海罂粟中分离的一种生物碱，具有镇咳、抗炎和支气管扩张作用。它是具有口服活性的磷酸二酯酶 4 选择性抑制剂。它还是非选择性的 α-肾上腺素受体拮抗剂，具有抗氧化和抗病毒活性。

S 3304 是一种新型的基质金属蛋白酶抑制剂，能够特异的抑制MMP-2和MMP-9的活性。

25(R,S)-Ruscogenin 能够调节 PI3K Akt mTOR 信号通路，抑制 MMP-2、MMP-9、uPA、VEGF 和 HIF-1α 的表达，阻碍肝癌转移。 它能够抑制 TLR4信号通路，减轻 LPS 诱导的肺内皮细胞凋亡。

NF-κB Activation Inhibitor III 是一种NF-kB 抑制剂，抑制 TNF-α 诱导的MMP-9上调，靶向抑制下游的MAPK p38，可用于靶向 TNF-α 介导的肿瘤侵袭和转移的化疗研究。

Histatin 5 TFA 抑制宿主基质金属蛋白酶MMP-2和MMP-9活性，IC50s 分别为 0.57 和 0.25 μM。

VPLSLYSG 是一种可被基质金属蛋白酶-9 (MMP-9)、MMP-1和MMP-2降解的八肽。VPLSLYSG 在MMP 底物中有潜在应用。

Chlorhexidine-d8 is intended for use as an internal standard for the quantification of chlorhexidine by GC- or LC-MS. Chlorhexidine is a bis(biguanide) antimicrobial disinfectant and antiseptic agent. It inhibits growth of clinical methicillin-resistant S. aureus (MRSA) isolates (MIC90 = 4 μg/ml). It is also active against canine isolates of MRSA, methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. pseudintermedius (MRSP), and methicillin-susceptible S. pseudintermedius (MSSP; MIC90s = 4, 2, 2, and 1 mg/L, respectively). Chlorhexidine inhibits growth of E. faecium strains (MICs = 1.2-19.6 μg/ml) and C. albicans (MIC = 5.15 μg/ml). It generates cations that bind to and destabilize the bacterial cell wall to induce death.6 Chlorhexidine also completely inhibits matrix metalloproteinase-2 (MMP-2) and MMP-9 when used at concentrations of 0.0001 and 0.002%, respectively, in a gelatin degradation assay. Formulations containing chlorhexidine have been used in antisept......

Hepcidin-1 (mouse) 是调控铁平衡的内源性多肽激素，通过上调TRAP、组织蛋白酶K和MMP-9的mRNA水平及增强TRAP-5b蛋白的分泌作用。此外，Hepcidin-1 (mouse) 降低FPN1蛋白水平并提升细胞内铁含量，且促进破骨细胞的分化。

22-(4′-py)-JA是久那霉素A的半合成衍生物，源自泰国蓝海绵（Xestospongia sp.）。该化合物显示出抗转移活性，能抑制AKT mTOR p70S6K信号通路，并阻断人脐静脉内皮细胞（HUVEC）中肿瘤细胞侵袭及管形成作用。它通过下调金属蛋白酶（MMP-2和MMP-9）、缺氧诱导因子1α（HIF-1α）和血管内皮生长因子（VEGF）来发挥作用。此外，22-(4′-py)-JA对非小细胞肺癌（NSCLC）显示出显著的抗癌效果。

ND-336 is a highly selective inhibitor ofMMP-2, MMP-9 and MMP-14. ND-336 accelerates diabetic wound healing by lowering inflammation and by enhancing angiogenesis and re-epithelialization of the wound.

Rac)-Tanomastat ((Rac)-BAY 12-9566) 是 Tanomastat 的外消旋体。其中 Tanomastat (BAY 12-9566) 是一种口服具有活力的、含锌羧基的非肽联苯基质金属蛋白酶(MMPs)抑制剂，能够抑制 MMP-2 (Ki: 11 nM)、MMP-3 (Ki: 143 nM)、MMP-9 (Ki: 301 nM)、MMP-13 (Ki: 1470 nM)。在几种实验性肿瘤模型中，Tanomastat 表现出抗侵袭和抗转移作用。

Coenzyme Q0 (CoQ0)，一种从Antrodia cinnamomea提取的口服醌类化合物，具备促进细胞凋亡(apoptosis)与自噬(autophagy)的作用。该化合物通过抑制HER-2 AKT mTOR信号通路，增强凋亡和自噬机制；同时，调控NFκB AP-1活化，提升Nrf2稳定性，从而缓解炎症及氧化还原失衡。此外，Coenzyme Q0还表现出抗血管生成特性，通过下降MMP-9 NF-κB并提升HO-1信号路径发挥作用。

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.

Dnp-PLGMWSR is a fluorogenic substrate for matrix metalloproteinase-2 (MMP-2) and MMP-9. The activity of MMP-2 and MMP-9 can be quantified by measuring tryptophan fluorescence that is unquenched upon peptide hydrolysis that removes the N-terminal dinitrophenol (Dnp) group.

Histatin 5 (TFA)(115966-68-2,free) (Histatin 5 (TFA)) 抑制宿主基质金属蛋白酶 MMP-2 和 MMP-9 的活性，IC50 分别为 0.57 和 0.25 μM。

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。

AZD1236 is a potent and reversible inhibitor of human MMP-9 and MMP-12 (IC50 = 4.5 and 6.1nM, respectively), with >10-fold selectivity to MMP-2 and MMP-13 and >350-fold selectivity to other members of the enzyme family. AZD1236 activity is approximately 20 to 50-fold lower at the rat, mouse, and guinea pig orthologues. In acute models of lung injury, AZD1236 inhibited the haemorrhage and inflammation induced by instillation of human MMP-12 into rat lungs by ~80% at 0.81mg/kg, and also abolished macrophage infiltration into BAL fluid induced by tobacco smoke inhalation in the mouse.

Aminopeptidase N (AP-N) inhibitor is a reversible inhibitor of AP-N/CD13 (IC50 = 25 μM). It is selective for AP-N/CD13 over matrix metalloproteinase-9 (MMP-9), angiotensin converting enzyme (ACE), neutral endopeptidase (NEP), γ-glutamyl transpeptidase, and the serine proteases dipeptidyl peptidase 4 (DPP-4) and cathepsin G at a concentration of 1 mM. AP-N inhibitor is non-cytotoxic to U937 cells at a concentration of 100 μM.