MMP-13 Inhibitor

Ageladine A dihydrochloride is an inhibitor of matrix metalloproteinase (MMP) isolated from the marine sponge Agelas nakamurai, possessing anti-angiogenic activity. Ageladine A dihydrochloride not only inhibits MMP-2 but also MMP-1, MMP-8, MMP-9, MMP-12, and MMP-13, with IC₅₀ values of 4.65 μM, 2.79 μM, 907.12 nM, 1.83 μM, 767.57 nM, and 1.09 μM, respectively. Additionally, Ageladine A dihydrochloride is a pH-sensitive membrane-permeable dye that emits fluorescence in the blue-green range upon UV excitation, featuring a maximum absorption peak at 370 nm. Furthermore, Ageladine A dihydrochloride serves as a reliable and stable fluorescent pH sensor for detecting changes in intracellular pH values.

CL-82198 hydrochloride is a selective inhibitor of MMP-13. CL-82198 hydrochloride binds to the entire S1’ pocket of MMP-13, which is the basis of its selectivity against MMP-1, MMP-9, and TACE.

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.

SC-77964 is a potent, selective and orally active matrix metalloprotease (MMP) inhibitor. SC-77964 shows IC₅₀ values < 0.1 nM against MMP-2, MMP-9, and MMP-13. SC-77964 can be used for the research of cancer and inflammation, such as melanoma.

WAY-170523 is a potent and selective MMP-13 (matrix metalloproteinase-13) inhibitor, with an IC₅₀ of 17 nM. WAY-170523 can directly attenuate ERK1/2 phosphorylation. WAY-170523 inhibits the invasion of PC-3 cells, can be used for prostate cancer 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.

SD-7300 (SC-81490) is an orally active inhibitor of MMP-2, MMP-9, and MMP-13 with K_i values ??of 0.03, 0.01, and 0.03 nM, respectively. SD-7300 can reduce the degradation of extracellular matrix by tumor cells, thereby inhibiting the invasion and metastasis of tumor cells. In addition, SD-7300 is also a dose-dependent inhibitor of mouse corneal angiogenesis and an inhibitor of interleukin-1-induced bovine cartilage degradation. SD-7300 can be used in breast cancer research.

2,5-Dihydroxy-4-methoxyacetophenone (compounds 3) can be isolated from the 80% methanol extract of roots of Cynanchum paniculatum Kitagawa. 2,5-Dihydroxy-4-methoxyacetophenone inhibits glutamate-induced cytotoxicity in hippocampal HT22 cell line. 2,5-Dihydroxy-4-methoxyacetophenone significantly inhibites MMP-13 expression in SW1353 cells, and have the potential for alleviating cartilage degradation.

WAY-151693, sulfonamide derivative of a hydroxamic acid, acts as a potent inhibitor of MMP13 in virtual screening.

Stevia Powder is a natural sweetener with antioxidant activity. Stevia Powder can downregulate pro fibrotic pathways in cirrhotic rats, including reduced hepatic myofibroblasts and decreased expression of matrix metalloproteinases MMP2 and MMP13, upregulate anti fibrotic molecule Smad7, prevent serum necrosis and elevated bile stasis markers, thereby inhibiting the development of liver fibrosis.