MMP-2 Inhibitor

α-Glucosylrutin, a flavonoid, is a potent antioxidant with free radical scavenging activity. α-Glucosylrutin reduces MMP-1 gene expression, protein expression, and enzyme activity, and reduces MMP-2 protein expression and enzyme activity in UVA-irradiated human dermal fibroblasts. α-Glucosylrutin prevents oxidative stress-induced intracellular tyrosine residue phosphorylation and counteracts intracellular thiol level depletion in human skin cells. α-Glucosylrutin is effective in the prevention of dermatologic diseases in which oxidative stress is of pathogenetic relevance, e.g. in polymorphous light eruption (PLE). α-Glucosylrutin can be used for the research of UV-induced skin photodamage/photoaging.

BI-4394 (MMP13-IN-3), a chemical probe, is a potent, selective, and orally active MMP-13 inhibitor (IC₅₀=1 nM) for the potential treatment of osteoarthritis. BI-4394 is >1000 selective over other MMPs.

AK-778-XXMU is a potent DNA binding inhibitor 2 (ID2) antagonist with a K_D of 129 nM. AK-778-XXMU can inhibit cell migration and invasion of glioma cell lines, induce apoptosis, and exhibits significant cancer-suppressing potency. AK-778-XXMU inhibits the ID2-KDR signaling axis, thereby down-regulating the downstream angiogenic factors (VEGFA) and invasion-related proteins (MMP2/9), and up-regulating the tumor suppressor factor (PTEN). AK-778-XXMU can be used for the study of glioma.

Prinomastat (AG3340) 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 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 crosses blood-brain barrier. Antitumor avtivity.

Ecliptasaponin A is an orally active pentacyclic triterpenoid saponin. Ecliptasaponin A exerts anti-tumor activity by activating ASK1/JNK pathway, inducing apoptosis and autophagy in lung cancer cells. Ecliptasaponin A exerts anti-inflammatory/anti-fibrotic effects and protects the cardiovascular system by inhibiting the HMGB1/TLR4/NF-κB pathway, and the expression of COX-2 and MMP-9. Ecliptasaponin A can enhance SOD activity, reduce MDA levels, and alleviate oxidative stress damage. Ecliptasaponin A exerts chondroprotective effects by inhibiting the expression of MMP13 and regulating inflammatory factors. Ecliptasaponin A improves ovarian function and regulates sex hormones by upregulating the expression of ESR1 receptors.

MMP13-IN-2 is a potent, selective and orally active MMP-13 inhibitor. MMP13-IN-2 exhibits excellent potency for MMP-13 (IC₅₀=0.036 nM) and selectivities (greater than 1,500-fold) over MMP-1, 3, 7, 8, 9, 14, and TACE. MMP13-IN-2 has the ability to block the release of collagen from cartilage in vitro. MMP13-IN-2 has the potential for collagenase related disease research.

MMP2-IN-1 is a moderate potenet MMP2 inhibitor with IC₅₀ of 6.8 µM. MMP2-IN-1 exhibits remarkable antiproliferative activity in certain cancer cells by arresting the cell cycle and inducing apoptosis.

Trilinolein is an orally active triglyceride that inhibits the PI3K/Akt, Ras/MEK/ERK signaling pathways, and MMP-2. Trilinolein can reduce oxidative stress, induce apoptosis, and inhibit cell migration. Trilinolein can be used in the research fields of cardiovascular disease, cerebrovascular disease (such as cerebral ischemia), and non-small cell lung cancer.

MMP-7-IN-2 is a potent and selective inhibitor of MMP7 with an IC₅₀ value of 16 nM. MMP-7-IN-2 can be used for the research of diseases such as cancer and fibrosis.

Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a K_i of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CL^pro inhibitor.

PT109 is an orally active, blood-brain barrier permeable multi-kinase inhibitor. By inhibiting PTBP1, PT109 promotes the switch of pyruvate kinase isoform from PKM2 to PKM1, thereby effectively inhibiting the proliferation and migration of glioblastoma multiforme and inducing its reprogramming into oligodendrocytes. PT109 also targets and regulates key signaling molecules such as JNK, SGK1, GSK3β to exert neuroprotective effects including promoting neurogenesis, inducing synapse formation and alleviating neuroinflammation. In Alzheimer's disease models, PT109 exhibits significant efficacy in improving spatial learning ability, along with excellent in vivo pharmacokinetic properties. PT109 can be used to investigate metabolic reprogramming of glioblastoma multiforme and neuroprotective mechanisms of Alzheimer's disease.

Viridicatol is a quinolone alkaloid with anti-inflammatory, antibacterial, antifungal, osteogenic and chondrogenic activities. Viridicatol reduces the phosphorylation levels of ERK, JNK, p38 and STAT6; inhibits MMP-2, MMP-9, NF-κB signaling pathway and PTP1B; downregulates genes related to mast cell activation; and binds to SHN3 to activate the Wnt/SHN3 signaling pathway. Viridicatol inhibits the expression of pro-inflammatory mediators and cytokines, and promotes osteogenic/chondrogenic differentiation. Viridicatol can be used in studies related to fibrosarcoma, allergy, bacterial infection, fungal infection and osteoporosis.

Regaloside C is an anti-inflammatory agent and antioxidant that scavenges ABTS and DPPH free radicals. Regaloside C targets multiple molecules including TNF-α, MMP-2, ERα, AKT1, TLR4 and HSP90-α. Regaloside C is applicable to research related to inflammatory diseases.

UK-370106 is a potent and highly selective MMP-3 (IC₅₀ of 23 nM) and MMP-12 (IC₅₀ of 42 nM) inhibitor with >1200-fold higher potency than MMP-1, MMP-2, MMP-9, and MMP-14, and about 100-fold than MMP-13 and MMP-8. UK-370106 potently inhibits cleavage of [³H]-fibronectin by MMP-3 (IC₅₀ of 320 nM) and has little effect on keratinocyte migration in vitro.

MMP-2/MMP-9-IN-1 is an N-sulfonyl amino acid derivative and matrix metalloproteinase MMP-9/MMP-2 inhibitor with IC₅₀ values of 0.24 μM and 0.31 μM for MMP-9 and MMP-2, respectively. MMP-2/MMP-9-IN-1 can be used for research on MMP-2/MMP-9-related cancers.

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.

Phenyl β-D-glucopyranoside is a component isolated from Phellodendron amurense, which has anti-inflammatory and anti-tumor activities. Phenyl β-D-glucopyranoside inhibits nitric oxide (NO) production, and the expression of iNOS and COX-2. Phenyl β-D-glucopyranoside also inhibits the nuclear translocation of NF-κB. Phenyl β-D-glucopyranoside inhibits the expression of pro-inflammatory cytokines and related genes.

PD-166793 is a potent, selective, orally active and wide-broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC₅₀=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC₅₀=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure.

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.