MMP-3 Inhibitor

(Rac)-Tanomastat ((Rac)-BAY 12-9566) is the racemate of Tanomastat. Tanomastat (BAY 12-9566) is an orally bioavailable, non-peptidic biphenyl matrix metalloproteinases (MMPs) inhibitor with a Zn-binding carboxyl group. The K_i values are 11, 143, 301, and 1470 nM for MMP-2, MMP-3, MMP-9, MMP-13 respectively. Tanomastat shows anti-invasive and antimetastatic activity in several experimental tumor models.

Berkeleyamide B is a dual matrix metalloproteinase-3 (MMP-3) and caspase-1 inhibitor. Berkeleyamide B is promising for research of cancers and inflammatory disease (e.g., rheumatoid arthritis).

Chamazulene, a natural compound, is an antioxidant-type inhibitor of leukotriene B4 formation.

Berkeleyamide C is a selective matrix metalloproteinase-3 (MMP-3) and caspase-1 inhibitor. Berkeleyamide C blocks MMP-3-mediated tumor cell invasion and metastasis, as well as the abnormal activation of inflammation and apoptosis related to caspase-1. Berkeleyamide C is promising for research of cancers and inflammation-related diseases.

F81-1144b is a MMP-1 and MMP-3 inhibitor with IC₅₀ values of 5 nM and 29 nM, respectively. F81-1144b reduces serum and hepatic triacylglycerol levels, decreases the secretion of very-low-density lipoprotein-triacylglycerol, inhibits de novo hepatic fatty acid synthesis, and lowers serum insulin and glucose levels. F81-1144b can be used for the research of hypertriglyceridemia.

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

BIM-46174 is a heterotrimeric G protein complex inhibitor. BIM-46174 blocks GPCR downstream signaling by trapping Gα proteins in a nucleotide-free pocket conformation, thereby inhibiting Gαq-mediated calcium release, Gαs-mediated cAMP production, and GPCR-regulated cancer cell invasion. In vitro, BIM-46174 effectively suppresses a variety of clinically multidrug-resistant cell lines and induces tumor cell apoptosis through activation of caspase-3 and PARP cleavage. BIM-46174 also inhibits activation of the Neu1-MMP-9-GPCR signaling platform and downstream NF-κB signaling, and is widely used in the study of cancer signaling pathways and inflammation-related research, including lung cancer, pancreatic cancer, breast cancer, melanoma, and leukemia.

CM-352 (compound 5) is an inhibitor of matrix metalloproteinases (MMPs) (MMP-3: IC₅₀=15 nM; MMP-10: IC₅₀=12 nM). CM-352 has significant antifibrinolytic activity (EC₅₀=0.7 nM) and can significantly prolong blood coagulation time. CM-352 can be used in anti-bleeding research.

Lixisenatide (Leu-¹³C₆,¹⁵N) TFA is the ¹³C- and ¹⁵N-labeled Lixisenatide (HY-P0119). Lixisenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide can be used for the researches of inflammation, metabolic disease, neurological disease and cardiovascular disease, such as rheumatoid arthritis, diabetes, Alzheimer's disease and atherosclerosis.

MMP3-IN-4 is a MMP-3 inhibitor with a pIC₅₀ value of 6.301. MMP3-IN-4 can be used in cancer research.

L 696418 is a MMP-3 inhibitor with a K_i value of 310 nM. L 696418 inhibits MMP-3 activity, thereby preventing the release of proteoglycans from cartilage. L 696418 reduces proteoglycan release in rabbit knee joints exposed to interleukin-1β (IL-1β). L 696418 can be used in research related to cartilage degradation.