MMP Inhibitor

RXP470.1 (RXP-470) is a potent, selective MMP-12 inhibitor with a K_i 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.

Kuwanon G is a flavonoid compound and an antagonist of the bombesin receptor. Kuwanon G has multiple activities such as bactericidal, anti-tumor, anti-inflammatory, antioxidant, anti-atherosclerotic, and neuroprotective effects. Kuwanon G exhibits strong antibacterial activity against oral pathogens, especially cariogenic bacteria and periodontal pathogens. Kuwanon G can induce apoptosis and inhibit proliferation, migration, and invasion of tumor cells. Kuwanon G can be used in the research of diseases such as gastric cancer and atherosclerosis.

Hydrangenol is an orally active antiphotoaging compound. It can be isolated from Hydrangea serrata leaves. Hydrangenol prevents wrinkle formation by reducing MMP and inflammatory cytokine expression and increasing moisturizing factors and antioxidant genes level.

MMP408 is a selective and orally effective inhibitor of MMP-12 with IC₅₀ values for human, mouse and rat MMP-12 of 2 nM, 160 nM and 3 μM respectively. MMP408 exhibits IC₅₀ value for human MMP-13 of 120 nM, and its activity against other MMPs is weak. MMP408 can alleviate inflammation, fibrosis and tissue remodeling by inhibiting MMP-12. MMP408 can be used in the research of chronic obstructive pulmonary disease and chronic sinusitis with nasal polyps.

Triolein-¹³C₃ is the ¹³C-labeled Triolein. Triolein is a symmetrical triacylglycerol, reduces MMP-1 upregulation, with strong antioxidant and anti-inflammatory properties.

20(R)-Ginsenoside Rh2 is an orally active protopanaxadiol-type saponin with multiple biological activities. 20(R)-Ginsenoside Rh2 exerts a significant inhibitory effect on non-small cell lung cancer and liver cancer by inducing cell cycle arrest and promoting apoptosis. 20(R)-Ginsenoside Rh2 exerts anti-γ-herpesvirus effects by inhibiting viral DNA replication. 20(R)-Ginsenoside Rh2 inhibits inflammatory mediators by reducing the levels of NO, PGE2, and ROS; it can delay skin photoaging by reducing ROS and inhibiting MMP-9/2 activity. 20(R)-Ginsenoside Rh2 accelerates the recovery after muscle injury by activating the Akt1/PKB signaling pathway. 20(R)-Ginsenoside Rh2 can inhibit osteoclast formation and exert an anti-osteoporosis effect.

MMPI-1154 is a promising novel cardio-cytoprotective imidazole-carboxylic acid (ICA) MMP-2 inhibitor(IC₅₀=6.6 μM) and can be used for the study of acute myocardial infarction. MMPI-1154 also inhibits the activity of MMP-13, MMP-1 and MMP-9 with IC₅₀s of 1.8 μM,10 μM, and 13 μM, respectively.

Imidapril (TA-6366 free base) is an orally active dual inhibitor of angiotensin-converting enzyme (ACE) and MMP-9. Imidapril inhibits lipopolysaccharide-induced phosphorylation of c-Jun, MKK4 and JNK in monocytes, and downregulates the production of specific inflammatory factors such as TNF-α and IP-10, thereby exerting anti-inflammatory activity. Imidapril also effectively ameliorates mesangial expansion and reduces urinary albumin excretion by inhibiting angiotensin AngII production, lowering glomerular pressure and oxidative stress, thus delaying disease progression. Imidapril can also directly bind to the active site of MMP-9 to inhibit gelatinase activity, and suppress the enlargement of cerebral aneurysms without altering systemic blood pressure. Imidapril is widely applicable to related studies on autoimmune glomerulonephritis, diabetic nephropathy, cerebral aneurysms and other conditions.

7-Methoxy-1-tetralone is a potent antitumor agent. 7-Methoxy-1-tetralone inhibits cancer cell proliferation and migration, and induces hepatocellular carcinoma cell (HCC) apoptosis. 7-Methoxy-1-tetralone decreased the protein levels of NF-κB, matrix metallopeptidase 2 (MMP2)/MMP9, and p-AKT. 7-Methoxy-1-tetralone showed antitumor activity in nude mice and had no effect on body weight and liver, spleen and organ index.

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.

DP-b99 is a blood-brain barrier-permeable inhibitor of CYP2C9 and MMP-9, with a K_i value of 4.655 μM against CYP2C9. DP-b99 inhibits CYP2C9 via apparent non-competitive inhibition, mainly chelates pathological Zn²⁺ in the membrane environment, attenuates the elevation of intracellular Zn²⁺ and Ca²⁺ levels, delays seizure onset and reduces seizure severity, and also prevents MMP-9-dependent dendritic spine remodeling, β-dystroglycan cleavage and gelatinase activity. DP-b99 can be used in the research of acute ischemic stroke, epileptogenesis and stroke.

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.

3-Hydroxy-2-pyrone (Compound 12d) is a metalloenzyme inhibitor. 3-Hydroxy-2-pyrone shows an inhibition rate of approximately 50% for matrix metalloproteinases (MMP) and the inhibition rate for non-heme iron enzyme 5-lipoxygenase (5-LOX) was over 70% at 1 mM. 3-Hydroxy-2-pyrone also has certain inhibitory activity against copper-dependent enzyme tyrosinase. 3-Hydroxy-2-pyrone can be used for the research of cancer, infection and inflammation.

Stigmasterol-d₆ is deuterium-labeled Stigmasterol (HY-N0131).

Triolein (Standard) is the analytical standard of Triolein. This product is intended for research and analytical applications. Triolein is a symmetric triacylglycerol that reduces upregulation of MMP-1 and has strong antioxidant and anti-inflammatory activities.

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.

ARP101 is a potent and selective inhibitor matrix metalloproteinase-2 (MMP-2). ARP101 induces autophagy-associated cell death in cancer cells. ARP101 is effective in inducing the formation of autophagosome and conversion of LC3I into LC3II.

β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties. β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca²⁺, and markedly decreases iNOS protein expression.

Salvianolic acid F is a KRAS inhibitor, especially for KRAS G12D. Salvianolic acid F inhibits NF-kB, MMP-9, and NO simultaneously. Salvianolic acid F inhibits cancer cell growth, invasion, and migration and induces apoptosis via the EP300/PI3K/AKT pathway in vitro. Salvianolic acid F inhibits the growth of KRAS-dependent lung cancer cells via the PI3K/AKT signaling pathway in vivo. Salvianolic acid F can be used in the research of various cancers, including KRAS G12D-driven non-small cell lung cancer (NSCLC) and ovarian cancer.