MMP-2 Inhibitor

Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC₅₀s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3, MMP-13 and MMP-9 with K_is of 0.05 nM, 0.3 nM, 0.03 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity.

Cipemastat is a potent, competitive inhibitor of human collagenases 1, 2 and 3 with K_is of 3.0, 4.4 and 3.4 nM, respectively.

CP-471474 is an orally active and pan MMP inhibitor, with IC₅₀ values of 1170 nM (MMP-1), 0.7 nM (MMP-2), 16 nM (MMP-3), 13 nM (MMP-9) and 0.9 nM (MMP-13), respectively.

MMP3 inhibitor 1 is a potent and highly selective MMP-3 inhibitor with an IC₅₀ of 1 nM.

XL-784 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, MMP-13, respectively.

YH-306 is an antitumor agent. YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. YH-306 significantly inhibits the migration and invasion of colorectal cancer cells. YH-306 potently suppresses uninhibited proliferation and induces cell apoptosis. YH-306 suppresses the activation of FAK, c-Src, paxillin, and PI3K, Rac1 and the expression of MMP2 and MMP9. YH-306 also inhibita actin-related protein (Arp2/3) complex-mediated actin polymerization.

Damulin B is a dammarane-type saponin found in Gynostemma pentaphyllum. Damulin B can inhibit cancer cell apoptosis, decrease mitochondrial membrane potential, inhibit ROS production and cause G0/G1 phase arrest. Damulin B can prevent Cisplatin (HY-17394)-induced acute kidney injury and induce hair growth. Damulin B shows anti-inflammation anti-diabetic and anti-obesity effect. Damulin B can be used for the researches of cancer, inflammation, metabolic disease, such as lung cancer, osteoarthritis and diabetes.

AGG-523 (PF-5212371) is an orally active, reversible, non-hydroxamate, zinc-binding selective inhibitor of ADAMTS4 and ADAMTS5 with IC₅₀ of <0.03 and 0.04 μM. AGG-523 also inhibits MMP-2, -8, 12 activity AGG-523 attenuates release of aggrecanase-generated ARG-aggrecan fragments into synovial fluid, reduces surgery-induced ARG-aggrecan release in rat joint models, and inhibits aggrecanase activity to slow cartilage degradation. AGG-523 can be used for the research of osteoarthritis.

HNHA is a potent HDAC inhibitor with an IC₅₀ of 100 nM. HNHA arrests the cell cycle at the G1/S phase via p21 induction. HNHA inhibits tumor growth and tumor neovascularization. HNHA may be a potent anti-cancer agent against breast cancer.

CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC₅₀s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis.

TP0597850 is a selective inhibitor of MMP2 (IC₅₀=0.22 nM). TP0597850 has a long MMP2 dissociation half-life (t_1/2=265 min).

BPHA is a potent and orally active MMP-2, MMP-9 and MMP-14 inhibitor with IC₅₀s of 12 nM, 16 nM and 17 nM, respectively. BPHA does not inhibit MMP-1, -3, and -7 (the IC₅₀s are 974, >1000, and 795 nM, respectively). BPHA has antiangiogenic and antitumor effects.

Hecogenin acetate is an orally active steroid saponin aglycone with extensive biological activities. Hecogenin acetate inhibits the phosphorylation of NF-κB and p38 MAPK signaling pathways, antagonizes TRPA1/TRPM8 channels, inhibits the production of pro-inflammatory cytokines, and has anti-inflammatory and analgesic effects. Hecogenin acetate inhibits the production of ROS and the activation of NLRP3 inflammasome; downregulates the expression of MMP-2, and has neuroprotective and anti-tumor activities. Hecogenin acetate enhances gastric mucosal defense and promotes ulcer healing. Hecogenin acetate can be used in combination with certain antibiotics to regulate bacterial efflux pumps and restore antibiotic sensitivity.

Isoviolanthin is a flavonoid glycoside. Isoviolanthin can be extracted from Dendrobium officinale. Isoviolanthin has a strong affinity for binding to KDM6B, CHAC2, ESCO2, and IPO4. Isoviolanthin decreases MMP-2 and MMP-9. Isoviolanthin inhibits TGF-β/Smad and PI3K/Akt/mTOR signaling pathways. Isoviolanthin increases Fhl3 expression. Isoviolanthin has cytoprotective effects. Isoviolanthin has anticancer activity against hepatocellular carcinoma.

2-(Methylamino) ethanol (N-Methylethanolamine) is an orally active Phospholipase D inhibitor and analog of Ethanolamine (HY-Y0524). 2-(Methylamino) ethanol reduces the mRNA levels of ACE, ppET-1 and ECE-1, and inhibits MMP-2 activity. 2-(Methylamino) ethanol inhibits Collagen synthesis. 2-(Methylamino) ethanol attenuates ventricular hypertrophy, prevents increased myocardial stiffness and hemodynamic deterioration. 2-(Methylamino) ethanol can capture industrial acid gases and react with carbon dioxide to form carbamates and bicarbonates. 2-(Methylamino) ethanol can be used in studies related to hypertensive heart failure (diastolic heart failure).

Nudol is a phenanthrene compound that has anti-cancer activity. Nudol inhibits cell proliferation, induces cell apoptosis. Nudol inhibits MMP-2M and MMP-9 activity (K_i: 988.9 nM, 1.76 μM, respectively). Nudol can be used in the research of cancers, such as osteosarcoma.

Linvemastat (Compound FC-4) is an orally active MMP-12 inhibitor (IC₅₀: < 10  nM) with high selectivity of MMP-1, -2, -3, -7, -9, -10 and -14. Linvemastat significantly attenuates lung fibrosis in Bleomycin (HY-108345) induced unilateral lung fibrosis mice model and potently reduces kidney damage, interstitial inflammation or fibrosis in kidney fibrosis model of unilateral ureteral occlusion. Linvemastat can be used for inflammatory diseases research, such as idiopathie pulmonary fibrosis (IPF), inflammatory bowel disease (IBD) and asthma.

MMP2-IN-2 (compound 42) is a potent and selective MMP-2 (matrix metalloproteinases) inhibitor, with an IC₅₀ of 4.2 μM. MMP2-IN-2 also shows inhibitory activity against MMP-13, MMP-9 and MMP-8, with IC₅₀ values of 12, 23.3, and 25 μM, respectively.

MMP-2 Inhibitor II (compound 2) is a selective MMP-2 inhibitor. The Kinetic parameters for MMP inhibition are 2.4 μM (MMP-2), 45 μM (MMP-1), and 379 μM (MMP-7), respectively.

CTTHWGFTLC, CYCLIC TFA is a cyclic peptide inhibitor for matrix metalloproteinases MMP-2 and MMP-9. The IC₅₀ value for MMP-9 is ~8 μM.