mmp-13

Acetamide, N-[2-[(5-chloro-2 methoxyphenyl)amino]-4'-methyl[4,5'-bithiazol]-2'-yl]-inhibits pro-matrix metalloproteinase activation and can be used to prevent, treat or ameliorate MMP9 and or MMP13-mediated syndromes.

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.

MMP-9 MMP-13 Inhibitor I is a dual inhibitor of MMP-9 and MMP-13 with IC50 of 0.9 nM for both enzymes. It is over 20 times more selective for MMP-9 MMP-13 than for other MMPs.

MMP-13 Substrate, a compound utilized in osteoarthritis (OA) research [1], functions as a substrate for MMP-13.

MMP-13-IN-1, with an IC50 value of 16 nM, is a potent and selective inhibitor of MMP-13, suitable for atherosclerosis research [1].

Marimastat (BB2516) (BB-2516) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor. MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM)and MMP-7 (IC50=13 nM).

DB04760 is a highly selective, non-zinc-chelating inhibitor of MMP-13 (IC50: 8 nM). DB04760 obviously decreases paclitaxel neurotoxicity and has anticancer activity.

CP-544439 is an orally active and potent MMP-13 inhibitor that prevents diet-induced obesity and inhibits adipogenesis in 3T3-L1 preadipocytes in mice, and can be used for the study of obesity.

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.

PD-166793 is an orally active, potent and selective MMP inhibitor with inhibitory effects on MMP-2, MMP-3 and MMP-13.PD-166793 ameliorates myocardial ischemia and reperfusion injury in a rat model of heart failure.PD-166793 is an orally active, potent and selective MMP inhibitor with inhibitory effects on MMP-2, MMP-3, and MMP-13.

Cytochalasin H ((16-Benzyl-5,12-dihydroxy-5,7,14-trimethyl-13-methylidene-18-oxo-17-azatricyclo[9.7.0.01,15]octadeca-3,9-dien-2-yl) acetate) is a potent inhibitor of actin incorporation into filaments.

PF-00356231 hydrochloride is an inhibitor of matrix metalloproteinase MMP-12 with IC50 of 1.4 μM.

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

XL-784 free base is a selective inhibitor of matrix metalloproteinases (MMP) with IC50 values of ~1900, 0.81, 120, 10.8, 18, and 0.56 nM for MMP-1, MMP-2, MMP-3, MMP-8, MMP-9, and 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).

CL-82198, a selective MMP-13 inhibitor, serves as a pharmacological intervention to halt the progression of osteoarthritis (OA). Its mechanism of action involves binding to the S1' pocket of MMP-13, ensuring its selectivity and preventing inhibition of other MMPs.

MMP13-IN-3 is >1000 selective over other MMPs. MMP13-IN-3 is an effective, selective, and orally active MMP-13 inhibitor (IC50=1 nM) for the potential treatment of osteoarthritis.

NF157 significantly decreases the expression of metalloproteinase (MMP)-3, MMP-13, which can be used in the treatment of osteoarthritis (OA). NF157 is a highly selective nanomolar P2Y11 antagonist (pKi: 7.35). The IC50s are 463 nM, 1811 µM, 170 µM for P2Y

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.

UK 356618 is a potent and selective inhibitor of matrix metalloprotease-3 (IC50: 5.9 nM).

SD-7300 (SC-81490) functions as an orally active inhibitor targeting MMP-2, MMP-9, and MMP-13, exhibiting potent inhibition with K_i values of 0.03, 0.01, and 0.03 nM, respectively. By inhibiting these metalloproteinases, SD-7300 effectively reduces extracellular matrix degradation by tumor cells, thereby curbing their invasion and metastasis. Additionally, this compound acts as a dose-dependent inhibitor of mouse corneal angiogenesis and prevents interleukin-1-induced degradation of bovine cartilage. SD-7300 is applicable in the study of breast cancer.

ALK5-IN-82 is a potent and selective inhibitor of activin receptor-like kinase 5 (ALK5), demonstrating an IC50 value of 9.1 nM. This compound effectively suppresses the expression of α-smooth muscle actin (α-SMA), collagen I, and the proteinases tissue inhibitor of metalloproteinase 1 (TIMP-1) and matrix metalloproteinase 13 (MMP-13) in human umbilical vein endothelial cells induced by transforming growth factor-β. ALK5-IN-82 shows potential for use in research related to cardiac fibrosis.

Collagenase Type III, an endopeptide matrix metalloproteinase MMP-13 derived from the bacterium Clostridium histolyticum, preferentially degrades type III collagen and is commonly used in sensitive tissues such as breast, tumor, and uterus due to its mild activity.

Broad spectrum MMP inhibitor (IC₅₀ 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.