mmp 12

MMP-12 Inhibitor 是一种选择性的 MMP-12 抑制剂，对人、小鼠、大鼠和绵羊 MMP-12 的 IC50 分别为 2、160、320 和 22.3 nM。

BAY-7598 is a potent, selective, and orally bioavailable MMP12 inhibitor (IC50s: 0.085, 0.67, and 1.1 nM for human murine rat MMP12).

CTS-1027 is a small molecule inhibitor of MMPs (IC50s: 0.3 nM, 0.5 nM for MMP2, MMP13). It has > 1,000 fold selectivity over MMP1.

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。

JG26 是一种强效的 ADAM17 抑制剂，对 ADAM8、ADAM17、ADAM10 和 MMP-12 均有抑制作用，其 IC50 值分别为 12 nM、1.9 nM、150 nM 和 9.4 nM，可用于研究机体免疫系统。

RXP470 is a potent and selective MMP-12 inhibitor (Ki 0.24 nM).

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.

MMP-7-IN-2 可作为一种具有选择性和有效性的 MMP7 抑制剂，可用于研究炎症反应和与血管相关的疾病。

TP0597850为MMP2选择性抑制剂，展现出卓越的亲和力（IC50=0.22 nM）和较长的MMP2解离半衰期（t1 2=265 min）。

PF 00356231 是一种特异性抑制剂 MMP-12，可用于治疗肺气肿和慢性阻塞性肺病 (COPD) 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.

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。

PF-00356231 hydrochloride 是基质金属蛋白酶 MMP-12 的抑制剂，IC50 为 1.4 μM。

TNO211为具备生物活性的肽，主要研究对象是基质金属蛋白酶（MMP），一类能够降解多种细胞外基质蛋白并调控诸多生物活性分子的肽链内切酶家族。MMP在细胞表面受体裂解、凋亡配体释放及趋化因子 细胞因子失活等过程中起作用，同时与细胞增殖、迁移（粘附 分散）、分化、血管生成、细胞凋亡及宿主防御等生物行为密切相关。TNO211可靶向MMP-2、8、12、13和14，包含MMP特定可裂解的Gly-Leu键，并具有EDANS DABCYL荧光标记，其荧光检测在监测内皮细胞培养基和患者滑液中的MMP活性方面表现出高灵敏度。吸光度 电磁场测量参数为340 490 nm。

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......

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.

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。

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.

LXJ-02 是一种有效抑制 EDPs EBP 肽-蛋白质相互作用的化合物，其与 EDPs 结合的 KD 为 117 μM。LXJ-02 可激活巨噬细胞-MMP-12 轴，增加 MMP-12 表达，从而降解 ECM 成分如弹性蛋白。

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).

MMP2-IN-2 是一种具有选择性的 MMP-2 (基质金属蛋白酶)抑制剂，具有潜在的抗癌抗肿瘤活性，抑制 MMP-13、MMP-9 和 MMP-8，可用于研究癌症和免疫疾病。

Tanomastat is an orally bioavailable and non-peptidic biphenyl matrix metalloproteinases inhibitor. For MMP-2, MMP-3, MMP-9, MMP-13 the Ki values are 11, 143, 301, and 1470 nM respectively.

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。

MMP408 是一种对MMP-12显示出抑制活性的化合物。