mmp-3 inhibitor

MMP-3 Inhibitor is a peptide matrix metalloproteinase-3 (MMP-3) inhibitor with a Ki value of 95 nM.MMP-3 inhibitor has anticancer and antitumor activity.

MMP-3 Inhibitor acetate is a cell-permeable and potent inhibitor of human MMP-3.

Matrix metalloproteinase-3 (MMP-3), also known as stromelysin-1, is a critical enzyme involved in tissue remodeling and repair through its role in degrading extracellular matrix proteins, facilitating cell migration. This enzyme has been implicated in various physiological processes including vascular remodeling associated with aneurysm formation, wound healing, the progression of atherosclerosis, and tumor initiation. MMP-3 inhibitor VIII, a cell-permeable sulfonamide-based hydroxamic acid, effectively inhibits MMP-3 by binding to its active site (Ki = 23 nM), thus blocking its enzymatic activity. Additionally, this inhibitor has been demonstrated to suppress the activity of mouse macrophage metalloelastase MME/MMP-12, with an IC50 value of 13 nM, highlighting its potential utility in research on tissue remodeling and disease processes involving MMPs.

GSK-3 inhibitor 1 is a GSK-3 inhibitor.

JAK1/2/3 Inhibitor 1 is a potent protein kinase inhibitor.JAK1/2/3 Inhibitor 1 has antitumor activity that inhibits the growth of a variety of cancer cell lines. It inhibits the growth of cancer cells by binding to the cancer cell backbone and inhibiting the production of new proteins.

GSK-3 Inhibitor 5 (4-Cyanophenacyl bromide) is a ketone derivative that is used as an intermediate in pharmaceuticals and organic synthesis, and inhibits glycogen synthase kinase 3 (GSK-3).

GSK-3 inhibitor 3 is a selective, orally active, brain-permeable GSK-3 inhibitor that inhibits GSK-3α and GSK-3β with IC50s of 0.35 nM and 0.25 nM, respectively.GSK-3 inhibitor 3 reduces the phosphorylation level of tau protein S396 with an IC50 of 10 nM in a triple transgenic mouse model of Alzheimer's disease. GSK-3 inhibitor 3 reduced the phosphorylation level of tau protein S396 in a triple transgenic mouse model of Alzheimer's disease, with an IC50 of 10 nM.GSK-3 inhibitor 3 can be used for the study of neurological diseases.

GSK-3 inhibitor 4 is an orally active and brain-permeable compound that acts as a triple inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM (CDK2), and 0.68 μM (CDK5). It effectively reduces Tau protein levels and can be used in the study of Alzheimer's disease.

Rac1 Inhibitor W56 acetate(1095179-01-3 free base) is a peptide comprising residues 45-60 of the guanine nucleotide exchange factor (GEF) recognition/activation site of Rac1. Rac1 Inhibitor W56 acetate(1095179-01-3 free base) selectively inhibits Rac1 interaction with Rac1-specific GEFs TrioN, GEF-H1 and Tiam1.

MMP-12 Inhibitor is a selective inhibitor of MMP-12 with IC50s of 2, 160, 320, and 22.3 nM for human, mouse, rat, and sheep MMP-12.

RIP2 Kinase Inhibitor 3 is a potent and selective inhibitor of RIP2, demonstrating an IC50 of 1 nM.

GSK-3 Inhibitor XIII, an ATP-competitive GSK-3 inhibitor (Ki: 24 nM), can be used to study diabetes and obesity.

mTOR inhibitor-3 is a selective mTOR inhibitor (Ki= 1.5 nM). mTOR inhibitor-3 inhibits mTORC1 and mTORC2 in cellular and in vivo experiments.

GSK 3 Inhibitor IX (6-BIO) is a selective reversible, ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex. It inhibits (GSK-3α/β)/CDK1/CDK5 activity with IC50 values of 5 nM/320 nM/83 nM, respectively.

Aurora kinase inhibitor-3 (Aurora Kinase Inhibitor III) is a potent inhibitor of Aurora A kinase (IC50 = 42 nM).1 It is selective for Aurora A over BMX, BTK, IGF-1R, c-Src, TRKB, SYK, and EGFR.

PRL-3 Inhibitor I (BR-1) is a phosphatase of regenerating liver 3 (PRL-3) inhibitor which blocks the migration and invasion of metastatic cancer cells.

Src Inhibitor 3 is an effective inhibitor of c-terminal Src kinase (IC50 <3 nM in CSK HTRF, <4 nM in Caliper assay). Src Inhibitor 3 increases T cell proliferation induced by T cell receptor signaling.

SCD1 inhibitor-3 (ML-270) is a highly effective and orally available compound that inhibits SCD1 with remarkable safety. SCD1 inhibitor-3 demonstrates strong potential for research in metabolic diseases, including obesity, type II diabetes, and dyslipidemia, as well as various skin conditions like acne and cancer.

MMP-7-IN-3 is a potent and selective MMP-7 inhibitor that effectively suppresses kidney fibrosis progression in a mouse model with unilateral ureteral obstruction [1].

MMP inhibitor I is a peptide inhibitor of matrix metalloproteinase-1 (MMP-1), MMP-2, and MMP-3 (IC50s = 1.3, 30, and 150 μM, respectively). It is selective for MMP-1, MMP-2, and MMP-3 over the proteases thermolysin, urease, trypsin, α-chymotrypsin, plasmin, and elastase at concentrations up to 4 mM.

MMP-9-IN-3 is an MMP-9 inhibitor (IC50: 5.56 nM) that forms hydrogen bonds with MMP-9. MMP-9-IN-3 inhibits AKT activity (IC50: 2.11 nM). mmp-9-IN-3 is cytotoxic and induces apoptosis. mmp-9-IN-3 can be used to study cancer.

XIAP BIR2 BIR2-3 inhibitor-1 (compound 3) serves as a potent dual inhibitor targeting BIR2 and BIR2-3 domains, with IC50 values of 1.9 nM and 0.8 nM, respectively. This compound is utilized in cancer research studies [1].

Compound 24, also known as YAP TAZ inhibitor-3, effectively inhibits YAP TAZ. It displays significant inhibitory activity against firefly luciferase, demonstrating an IC 50 value of less than 0.1 μM [1].

Chitin Synthase Inhibitor 3 (Compound 2d) is a potent inhibitor of chitin synthase, exhibiting an IC50 value of 0.16 mM and demonstrating antifungal activity with a minimum inhibitory concentration (MIC) of 1 μg/mL against Candida albicans [1].

JNK3 Inhibitor-3 (compound 15g) is a selective, blood-brain barrier permeable, and orally active inhibitor of c-Jun N-terminal kinase 3 (JNK3) with IC50 values of 147.8 nM, 44.0 nM, and 4.1 nM against JNK1, JNK2, and JNK3, respectively. This compound has been shown to significantly enhance memory in mouse models of dementia and is utilized in Alzheimer’s disease research [1].

KRAS inhibitor-3, an efficacious inhibitor of both wild-type (WT) and oncogenic KRAS mutations, exhibits high-affinity binding (K D: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, and 0.74 μM for KRAS Q61H). Additionally, it impedes the interaction between KRAS and Raf, highlighting its potential as a targeted therapeutic agent in KRAS-mutant cancers.

PI4KIII beta inhibitor 3 is a novel, highly effective inhibitor of PI4KIIIβ with an IC50 of 5.7 nM.

ChoKα Inhibitor-3, a sulfur-containing choline kinase inhibitor, effectively inhibits HChoK α1 with an IC50 value of 0.66 μM and possesses the capability to induce apoptosis. This compound is utilized in cancer research [1].

PI3K mTOR Inhibitor-3 (compound 12) is an imidazoline compound with potent dual inhibition of PI3K and mTOR, exhibiting notable anti-cancer activity [1].

Topoisomerase I II inhibitor 3 (compound 7) is a potent dual inhibitor of topoisomerase I (Topo I) and II (Topo II) that inhibits the PI3K Akt mTOR signaling pathway, subsequently inhibiting cell proliferation, invasion, and migration, and inducing apoptosis. This compound has research value in liver cancer.

Glutaminyl Cyclase Inhibitor 3, a designed anti-Alzheimer’s compound, is a potent human Glutaminyl Cyclase (GC) inhibitor (IC50: 4.5 nM). It significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions.

HIV-1 integrase inhibitor 3 is an HIV-1 integrase strand transfer (INST) inhibitor with an IC50 of 2.7 nM.

KRas G12C inhibitor 3 is a compound that specifically inhibits the KRas G12C mutation.

α-Synuclein inhibitor 3 (Compound 7g) is a potent inhibitor of α-synuclein (α-Syn) aggregation, with potential applications in Parkinson's disease research [1].

Topoisomerase II inhibitor 3 (Compound 6 h) is an acridone derivative acting as a Type II DNA topoisomerase (topo II) inhibitor. It specifically targets topo IIα β subtypes, with IC50 values of 0.17 μM for topo IIα and 0.23 μM for topo IIβ, causing significant DNA damage and inducing apoptosis by triggering the loss of mitochondrial membrane potential [1].

Compounds 17o (IC50: 14.0 nM, NCI-H460) and 17p (IC50: 2.9 nM, NCI-H460) with furan moieties showed potent cytotoxic effects at the nanomolar level against various human cancer cell lines.

Compound 5a, also known as DPP-4 inhibitor 3, is a powerful dipeptidyl peptidase IV (DPP-IV) inhibitor, demonstrating an IC50 value of 0.75 nM. It exhibits outstanding antioxidant and insulinotropic activity [1].

Schnurri-3 inhibitor-1, a potent inhibitor of schnurri-3, is an essential regulator of bone formation in adults that can be used in osteoporosis research. Schnurri-3 inhibitor-1 can inhibit Shn3 with EF1alpha promoter in osteoblast cell line Shn3FFL (AC50 = 2.09 μM) [1].

EGFR kinase inhibitor 3 (compound 2) serves as a dual-action inhibitor targeting both ATP and allosteric sites of the EGFR kinase, exhibiting potent IC50 values of less than 10 nM for wild-type EGFR, 1.5 nM for the L858R mutation, 0.059 nM for the L858R T790M mutation, and 0.064 nM for the L858R T790M C797S mutation. It is classified as a C-linked inhibitor [1].

IGF-1R Inhibitor-3 (Compound C11) serves as an allosteric inhibitor targeting the kinase of insulin-like growth factor receptor 1 (IGF-1R), exhibiting an IC50 value of 0.2 μM [1].

Necrosis Inhibitor 3 (compound B3) effectively inhibits necrosis, demonstrating an IC50 of 0.29 nM in HT29 cells [1].

Cyclophilin inhibitor 3 (compound 7c), a potent inhibitor of cyclophilin A (CypA), exhibited potent anti-HCV effects with an EC50 value of 4.2 μM.

Prostaglandin E2 (PGE2) inhibitor 3 is a selective inhibitor targeting microsomal prostaglandin E synthase-1 (mPGES-1; IC50 = 0.2 µM), demonstrating greater selectivity for mPGES-1 over COX-1, COX-2, 5-lipoxygenase (5-LO), and soluble epoxide hydrolase (sEH) in assays at 10 µM. This compound effectively reduces IL-1β-induced PGE2 production in A549 cells and decreases LPS-induced IL-6 and PGE2 in J774A.1 macrophages at concentrations of 10 and 1 µM, respectively. Additionally, it blocks the production of 5-LO-derived products, including leukotriene B4 (LTB4) and 5-H(p)ETE, in response to calcium ionophore A23187 alone or combined with arachidonic acid, with IC50 values of 4.9 and 5.2 µM, respectively. When administered in vivo at doses of 10 mg/kg, PGE2 inhibitor 3 effectively prevents leukocyte infiltration in a mouse model of zymosan-induced peritonitis.

Z-DEVD-FMK, a Caspase-3 Inhibitor, is an irreversible, cell-permeable inhibitor of caspase-3/CPP32 that impedes tumor cell apoptosis. In vivo studies show it offers neuroprotection in rat hippocampi post-seizures and considerably diminishes post-traumatic apoptosis, enhancing neurological recovery in rats before and after traumatic brain injury induction.

IDH1 Inhibitor 3 is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor (IC50: 45 nM for IDH1R132H).

UCK2 Inhibitor-3 is a non-competitive inhibitor of uridine-cytidine kinase 2 (UCK2), a pivotal enzyme in the pyrimidine salvage pathway, with an IC50 value of 16.6 μM. UCK2 can partially substitute for dihydroorotate dehydrogenase (DHODH) in infected or rapidly dividing cells, aiding uridine salvage. Additionally, UCK2 Inhibitor-3 inhibits DNA polymerase eta and kappa, with IC50 values of 56 μM and 16 μM, respectively.

BRM BRG1 ATP Inhibitor-3 is a potent inhibitor targeting both BRM and BRG1 components of the BAF complex, with IC50 values of 10.4 nM for BRM and 19.3 nM for BRG1, and holds potential for research in cancer and BAF complex-related disorders.

P-gp Inhibitor 3, an effective P-glycoprotein (P-gp) inhibitor, activates P-gp ATPase to inhibit P-gp's efflux function. It demonstrates a relatively stronger multidrug resistance (MDR) reversal ability, thereby enhancing the anti-tumor efficacy of Paclitaxel.