MMP Inhibitor

Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator.

TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC₅₀ of 20 μM for MMP. TAPI-2 blocks the entry of infectious SARS-CoV.

Otaplimastat (SP-8203), a matrix metalloproteinase (MMP) inhibitor, blocks N-methyl-D-aspartate (NMDA) receptor-mediated excitotoxicity in a competitive manner. Otaplimastat also exhibits anti-oxidant activity. Otaplimastat can be used for the research of brain ischemic injury.

MMP-9-IN-13 (Example 1) is a selective inhibitor of human MMP9 with an IC₅₀ value of 0.02 nM. MMP-9-IN-13 can be used in the research of ocular surface.

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

GI254023X is a potent MMP9 and ADAM10 inhibitor with IC₅₀s of 2.5 and 5.3 nM, respectively.

Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy.

Batimastat is a potent broad spectrum MMP inhibitor with IC₅₀ of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.

NSC 405020 is a specific MMP14 inhibitor. NSC 405020 can directly interact with the hemopexin domain of MMP14. NSC 405020 reduces the expression of full length and active cleaved Notch3 (NICD3). NSC 405020 can be used to research vestibular schwannoma, hemostasis and thrombosis.

Arctigenin ((-)-Arctigenin), a biologically active lignan, can be used as an antitumor agent. Arctigenin exhibits potent antioxidant, anti-inflammatory and antiviral (influenza A virus) activities. Arctigenin can be used for the research of metabolic disorders, and central nervous system dysfunctions.

(-)-Epigallocatechin (Epigallocatechin) is the most abundant flavonoid in green tea, can bind to unfolded native polypeptides and prevent conversion to amyloid fibrils.

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 K_i of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with K_i 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.

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.

JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC₅₀ of 440 nM.

CL-82198 is a selective inhibitor of MMP-13. CL-82198 binds to the entire S1’ pocket of MMP-13, which is the basis for its selectivity towards MMP-13 and the lack of inhibitory activities against other MMPs. CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression.

Incyclinide (CMT-3, COL-3) is a matrix metalloproteinase (MMP) inhibitor and inhibiting angiogenesis, tumor growth and invasion, and metastasis.

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.

cyclo(RLsKDK) (TFA) (BK-1361 (TFA)) is a specific inhibitor of metalloproteinase ADAM8 with an IC₅₀ value of 182 nM. cyclo(RLsKDK) (TFA) has potential applications in inflammatory diseases and cancer.

Kukoamine B, a spermine alkaloid, is a potent dual LPS and CpG DNA inhibitor with K_d values of 1.23 µM and 0.66 µM, respectively. Kukoamine B exerts anti-inflammatory, anti-diabetic, anti-oxidant, anti-osteoporotic and neuroprotective effects. Kukoamine B has the potential for the study of sepsis.

α-solanine, a bioactive component and one of the major steroidal glycoalkaloids in Solanum nigrum, has been observed to inhibit growth and induce apoptosis in cancer cells.