Triolein-d5 is the deuterium labeled Triolein. Triolein is a symmetrical triacylglycerol, reduces MMP-1 upregulation, with strong antioxidant and anti-inflammatory properties[1].
MMP Inhibitor II (compound 4e) is a potent, reversible pan-MMP inhibitor with IC50 values of 24 nM, 18.4 nM, 30 nM, and 2.7 nM for MMP-1,MMP-3, MMP-7, and MMP-9, respectively[1].
Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor[1].
Mca-P-Cha-G-Nva-HA-Dap(DNP)-NH2 is a fluorogenic substrate for matrix metalloproteinase-1 (MMP-1), MMP-3, and MMP-26. Mca-P-Cha-G-Nva-HA-Dap(DNP)-NH2 can be used to quantify MMP-1, MMP-3 and MMP-26 activity[1][2].
(S,S)-TAPI-1 is an isomer of TAPI-1. TAPI-1 is a TACE (ADAM17) inhibitor and blocks the shedding of several cell surface proteins. TAPI-1 is also a metalloproteinase (MMP) inhibitor[1][2].
PG 116800 (PG 530742) is an orally avtive MMP inhibitor. PG 116800 has high affinity for MMP-2, -3, -8, -9, -13, and -14, while having substantially lower affinity for MMP-1 and -7. PG 116800 can be used for knee osteoarthritis research[1].
MMP-8 inhibitor-1 (compound 21), a hydroxamic acid derivative, is a potent MMP-8 inhibitor without significant oral bioavailability[1].
Lucideric acid A is a natural compound isolated from Ganoderma lucidum, inhibits PMA-induced MMP-9 activity, with anti-invasive effect on hepatoma cells[1].
(R)-ND-336 is a potent and selective MMP-9 inhibitor with a Ki of 19 nM. (R)-ND-336 inhibits MMP-2 (Ki=127 nM) and MMP-14 (Ki=119 nM). (R)-ND-336 has the potential for diabetic foot ulcers (DFUs) research[1].
Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment [1]. Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex[2].
Anticancer agent 65 (compound 4c) shows excellent activity in cancer cell lines, especially A549 cells, with an IC50 of 1.07 μM. Anticancer agent 65 induces S-phase arrest in A549 cells and increases the expression level of p53 and p21. Anticancer agent 65 causes apoptosis, ROS generation and collapse of MMP in A549 cells[1].
JG26 is an ADAM17 inhibitor, with IC50 values of 12 nM, 1.9 nM, 150 nM and 9.4 nM for ADAM8, ADAM17, ADAM10 and MMP-12, respectively[1].
cis-ACCP is an orally active antimetastatic matrix metalloproteinase-2 (MMP-2) selective inhibitor. cis-ACCP can inhibit MMP-2 and MMP-9 with IC50 values of 4 μM and 20 μM, respectively. cis-ACCP can be used for the research of a variety of chronic diseases[1].
Licoricidin (LCD) is isolated from Glycyrrhiza uralensis Fisch, possesses anti-cancer activities.Licoricidin (LCD) inhibit SW480 cells (IC50=7.2 μM) by inducing cycle arrest, apoptosis and autophagy, and is a potential chemopreventive or chemotherapeutic agent against colorectal cancer[1].Licoricidin (LCD) inhibits Lung Metastasis by inhibition of tumor angiogenesis and lymphangiogenesis as well as changes in the local microenvironment of tumor tissues the anticarcinogenic effect[1].licoricidin enhanced gemcitabine-induced cytotoxicity in Osteosarcoma (OS) cells by inactivation of the Akt and NF-κB pathways in vitro and in vivo[3]. Licoricidin blocks UVA-induced photoaging via ROS scavenging, limits the activity of MMP-1, it can be considered as an active ingredient in new topically applied anti-ageing formulations[4].
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities[1][2][3][4][5].
BT1718 is a bicyclic anticancer peptide targeting MT1-MMP. BT1718 uses MT1-MMP to target tumors and promote delivery of the cytotoxic payload Mertansine (HY-19792). BT1718 is a bicycle toxin conjugate with a KD value of 3 nM. MT1-MMP is overexpressed in a variety of advanced solid tumors, including triple-negative breast cancer (TNBC), non-small cell lung cancer[1][2].
PI3K/AKT-IN-2 (Compound 12c) is a PI3K and AKT inhibitor. PI3K/AKT-IN-2 blocks the epithelial-mesenchymal transition (EMT) and induces apoptosis. PI3K/AKT-IN-2 inhibits the polymerization of tubulin[1].
D-Isofloridoside, one of the polysaccharide precursors, has the activity of scavenging free radicals, inhibiting ROS expression, and inhibiting MMP-2 and MMP-9[1][2].
20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity[1][2][3].
RXP470.1 (RXP-470) is a potent, selective MMP-12 inhibitor with a Ki of 0.2 nM against human MMP-12. RXP470.1 is 2 to 4 orders of magnitude less potent against other MMPs. RXP470.1 significantly reduces atherosclerotic plaque cross-sectional area in mouse. RXP470.1 results in less complex plaques with increased smooth muscle cell:macrophage ratio, less macrophage apoptosis, increased cap thickness, smaller necrotic cores, and decreased incidence of calcification[1].
Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
MMP-13-IN-1 is a potent and selective inhibitor of MMP-13 with a IC50 value of 16 nM. MMP-13-in-1 can be used for atherosclerosis research[1].
DB04760 (compound 4) is a potent, highly selective, non-zinc-chelating MMP-13 inhibitor with an IC50 of 8 nM[1]. DB04760 significantly reduces paclitaxel neurotoxicity and has anticancer activity[2].
ROCK2-IN-7 is a kinase inhibitor targeting to ROCK2. ROCK2-IN-7 inhibits ROCK2/pSTAT3 Signaling. ROCK2-IN-7 suppresses systemic immunity activation and attenuates inflammation in psoriasis model[1].
TAPI-0 is a TACE (TNF-α converting enzyme; ADAM17) inhibitor with an IC50 of 100 nM. TAPI-0 is a MMP inhibitor and also attenuates TNF-α processing[1][2].
ND-322 HCl is a selective inhibitor of MT1-MMP and MMP2 and reduces in vitro melanoma cell growth, migration and invasion.
PythiDC is a selective collagen prolyl 4-hydroxylase (CP4H1) inhibitor with an IC50 value of 4.0 μM. PythiDC can be used as a CP4H probe and also can be used for the development of a new class of antifibrotic and antimetastatic agents[1].
Feprazone (DA2370; Prenazone), an analogue of Phenylbutazone (HY-B0230), is a nonsteroidal anti-inflammatory agent with analgesic and antipyretic activities. Feprazone acts by inhibiting the activity of cyclooxygenase (COX)-2. Feprazone ameliorates free fatty acid (FFA)-induced oxidative stress by reducing the production of mitochondrial reactive oxygen species (ROS). Feprazone can decrease the expression of MMP-2 and MMP-9. Besides, Feprazone can suppress adipogenesis and increase lipolysis in differentiating 3 T3-L1 cells. Feprazone also can be used to research atherosclerosis and obesity[1][2][3].
Meloxicam sodium is a non-steroidal anti-inflammatory agent, inhibits COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and COX-1, respectively[1].
Ilomastat (Galardin; GM6001) is a broad spectrum matrix metalloprotease (MMP) inhibitor, with Ki of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 0.36 nM for MMP-1/2/3/7/8/9/12/14/26, respectively.