MMP Inhibitor

Levamlodipine besylate Hemipentahydrate is an orally active L-type calcium channel blocker and MMP-9 modulator with high permeability and retention properties. Levamlodipine besylate Hemipentahydrate significantly enhances plaque stability and improves lipid profiles by reducing blood pressure, decreasing systolic blood pressure variability, and inhibiting MMP-9 expression in atherosclerotic plaques. Levamlodipine besylate Hemipentahydrate not only alleviates cardiac and aortic hypertrophy and prevents renal atrophy, but also produces synergistic effects in blood pressure reduction and organ protection when combined with bisoprolol (HY-129029). Levamlodipine besylate Hemipentahydrate exerts no significant inhibitory effect on abdominal aortic intimal hyperplasia. When excessively accumulated in the epidermis, Levamlodipine besylate Hemipentahydrate may induce changes in keratin structure, impair the skin barrier and trigger inflammation; long-term use further exacerbates skin irritation caused by local administration. Levamlodipine besylate Hemipentahydrate can be used in research related to hypertension and atherosclerosis.

Apratastat (Standard) is the analytical standard of Apratastat. This product is intended for research and analytical applications. Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC). Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Indinavir-¹³C₄,¹⁵N (MK-639 (free base)-¹³C₄,¹⁵N) is ¹³C and ¹⁵N labeled Indinavir. 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.

MMP3-IN-4 is a MMP-3 inhibitor with a pIC₅₀ value of 6.301. MMP3-IN-4 can be used in cancer research.

Phillygenin-O-β-glucosaminide is an orally active Nrf2 inducer and NF-κB inhibitor that inhibits osteoclast differentiation and ROS production by promoting Nrf2 nuclear translocation, suppressing NF-κB and JNK phosphorylation, and downregulating NFATc1, c-Fos, MMP9, and CTSK expression. Phillygenin-O-β-glucosaminide can be used for research on osteoarthritis.

CZh226 is a selective PAK4 inhibitor with an IC₅₀ of 0.0111 μM and a K_i of 0.009 μM. CZh226 functionally inhibits PAK4 activity and reduces the phosphorylation level of downstream signaling molecules. CZh226 inhibits the migration and invasion of tumor cells. CZh226 is applicable to lung cancer-related research.

Aderbasib (Standard) is the analytical standard of Aderbasib (HY-10293). This product is intended for research and analytical applications. Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2+ breast cancer, gliomas, et al.

Talopeptin is a metal protease inhibitor that can be produced by the streptomyces MK-23.

o-Phenanthroline (1,10-Phenanthroline) monohydrate, a metal chelator, prevents the induction of chromosomal aberrations in streptozotocin-treated cells. o-Phenanthroline monohydrate forms a red chelate with Fe2+ that absorbs maximally at 510 nm. o-Phenanthroline (1,10-Phenanthroline) monohydrate is also a MMP inhibitor.

Tianeptine sodium salt (Standard) is the analytical standard of Tianeptine sodium salt (HY-90003A). This product is intended for research and analytical applications. Tianeptine sodium salt is an atypical antidepressant. Tianeptine sodium salt is a moderate-intensity agonist of the μ-opioid receptor (MOR), and to a lesser extent, is an agonist of the δ-opioid receptor (DOR). Tianeptine sodium salt is a glutamate modulator that can enhance AMPA receptor and antagonize NMDA receptor. Tianeptine sodium salt increases sensitivity of the α1 adrenergic receptor, which only manifests in chronic treatment. Tianeptine sodium salt exerts neuroprotective effects under stress/inflammation-induced conditions, exhibiting anti-inflammatory and antioxidant properties. Tianeptine sodium salt inhibits MMP-9 by suppressing the PI3K/Akt-mediated NF-κB pathway. Tianeptine sodium salt can be used to alleviate symptoms of depression and anxiety, but does not cause sedative effects.

CGS-25015 is a mercapto-containing metalloprotease inhibitor that inhibits endothelin-converting enzyme (ECE). CGS-25015 inhibits ECE activity with an IC₅₀ of 2.6 μM in porcine coronary artery smooth muscle preparations, and an IC₅₀ of 18 μM in partially purified porcine aortic endothelial cell ECE preparations. CGS-25015 inhibits endothelin production and the resulting vascular smooth muscle contractile response.

Tremulacin is a 5-LOX inhibitor. Tremulacin reduces the biosynthesis of LTB₄ and slow-reacting substances of anaphylaxis. Tremulacin alleviates carrageenan-induced paw edema in rats, croton oil-induced ear edema in mice, and acetic acid-induced writhing response in mice. Tremulacin inhibits TNF-α-stimulated ROS production and MMP-1 expression, and promotes collagen secretion in human dermal fibroblasts. Tremulacin is investigated for studies on inflammation-related diseases.

Anethole (Standard) is the analytical standard of Anethole. This product is intended for research and analytical applications. Anethole is a type of orally active aromatic compound that is widely found in nature and used as a flavoring agent. Anethole possesses anticancer, anti-inflammatory, antioxidant, antibacterial, antifungal, anesthetic, estrogenic, central nervous system depressant, hypnotic, insecticidal, and gastroprotective effects. Anethole can be used in the study of oxidative stress-related skin diseases and prostate cancer.

Z-Acp-leu-metyr-MA (Collagenase inhibitor CI-2) is a mammalian tissue collagenase inhibitor, with an IC₅₀ of 200 μM against human rheumatoid synovial collagenase, 30 μM against mouse bone collagenase, 60 μM against rabbit bone proteoglycanase, 25 μM against mouse bone neutral protease, and >100 μM against rabbit macrophage neutral protease. Z-Acp-leu-metyr-MA inhibits parathyroid hormone-induced bone collagen matrix resorption in cultured embryonic mouse calvariae.

L-Val-P is a potent leucine aminopeptidase (LAP) inhibitor with a K_i of 0.15 μM. L-Val-P is promising for research of HIV infection, inflammation, eye lens cataract and cancer.

KP-457 (Standard) is the analytical standard of KP-457 (HY-110397). This product is intended for research and analytical applications. KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC₅₀s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.

Isofraxidin (Standard) is the analytical standard of Isofraxidin. This product is intended for research and analytical applications. Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation.

Homorisedronate (NE-58051) is a MMP inhibitor with high bone mineral affinity but low bone antiresorptive activity in vivo. Homorisedronate inhibits the proteolytic activity of MMP-2, MMP-9, and MMP-12 through zinc chelation and phosphonate groups, with IC₅₀ values of 40 μM, 160 μM, and 80 μM for human MMP-2, mouse MMP-9, and rabbit MMP-12, respectively. Homorisedronate inhibits breast cancer and melanoma cell proliferation without inducing MRONJ-like lesions, altering osteoclast activity, or changing serum TRAcP-5b levels. Homorisedronate is suitable for research related to breast cancer and melanoma.

Hinokiflavone is a novel modulator of pre-mRNA splicing activity extracted from plants with anti-inflammatory, anti-tumor and antiviral activities. Hinokiflavone is also a potent inhibitor for matrix metalloproteinases (MMPs). Hinokiflavone attenuates the virulence of Methicillin (HY-121544)-resistant staphylococcus aureus by inhibiting caseinolytic protease P (ClpP) with an IC50 value of 34.36 mg/mL. Hinokiflavone induces apoptosis via the reactive oxygen species-mitochondria-mediated apoptotic pathway and inhibits tumor cell migration and invasion. Hinokiflavone is a SUMO protease inhibitor against sentrin-specific protease 1 (SENP1) activity.

Abametapir (Standard) is the analytical standard of Abametapir. This product is intended for research and analytical applications. Abametapir is a metalloproteinase (MMP) inhibitor which is able to target metalloproteinases critical to egg hatching and louse development. Abametapir can inhibit hatching of both head and body louse.