MMP-1-IN-1

MMP-1-IN-1 is a highly potent MMP-1 inhibitor with an IC 50 of 0.034 μM .

Astragaloside IV (AS-IV), an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells. Astragaloside IV is a bioactive saponin first isolated from the dried plant roots of the genus Astragalus, which is used in traditional Chinese medicine.1 It dose-dependently inhibits human adenovirus type 3 (HAdV-3) in A549 cells (IC50 = 23 μM; LC50 = 865 μM).It inhibits replication of HAdV-3 and decreases HAdV-3-induced apoptosis. It has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems. In particular, it reduces myocardial infarct size in dogs when administered prior to coronary ligation and reduces reperfusion arrhythmias in isolated rat hearts.

MMP-9-IN-1 is an inhibitor of specific matrix metalloproteinase-9 (MMP-9).

Collagenase Type I is a proteolytic enzyme that primarily targets collagen and is able to break down peptide bonds in collagen. Collagenase is used as a potential therapeutic option to break up the herniated disc material, thereby reducing compression of nearby nerves. Collagenase may aid in the breakdown and reorganization of excessive scar tissue, potentially improving tissue function and appearance. Collagenase has the potential to treat intervertebral disc herniation, keloid, fat mass, lipoma, as well as Peyronie's disease and palmar fibromatosis.

XL-784 is a selective inhibitor of matrix metalloproteinases (MMPs) with IC50 values of approximately 1900, 0.81, 120, 10.8, 18, and 0.56 nM for MMP-1, MMP-2, MMP-3, MMP-8, MMP-9, and MMP-13, respectively. XL-784 demonstrates potential in a broad range of cancer research applications due to its capability to modulate extracellular matrix remodeling, tumor invasion, and metastasis.

ARP-100 (MMP-2 Inhibitor III) is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with the S1' pocket of MMP-2 and exhibits anti-invasive properties in an in vitro invasion Matrigel model. ARP-100 has low inhibitory activity against MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM) and MMP-9 (0.2 μM)[1][2].

DBCO-NHCO-PEG4-NHS ester is a DBCO-containing PEGylated active ester linker that combines NHS ester reactivity toward primary amines with strain-promoted azide-alkyne cycloaddition capability. It enables efficient bioconjugation through amide coupling and copper-free click reaction with azide groups. The PEG4 spacer provides hydrophilicity and tunable linker length, making it widely used in PROTAC and antibody-drug conjugate (ADC) construction.

MMP13-IN-3 is >1000 selective over other MMPs. MMP13-IN-3 is an effective, selective, and orally active MMP-13 inhibitor (IC50=1 nM) for the potential treatment of osteoarthritis.

SD-7300 (SC-81490) functions as an orally active inhibitor targeting MMP-2, MMP-9, and MMP-13, exhibiting potent inhibition with K_i values of 0.03, 0.01, and 0.03 nM, respectively. By inhibiting these metalloproteinases, SD-7300 effectively reduces extracellular matrix degradation by tumor cells, thereby curbing their invasion and metastasis. Additionally, this compound acts as a dose-dependent inhibitor of mouse corneal angiogenesis and prevents interleukin-1-induced degradation of bovine cartilage. SD-7300 is applicable in the study of breast cancer.

ALK5-IN-82 is a potent and selective inhibitor of activin receptor-like kinase 5 (ALK5), demonstrating an IC50 value of 9.1 nM. This compound effectively suppresses the expression of α-smooth muscle actin (α-SMA), collagen I, and the proteinases tissue inhibitor of metalloproteinase 1 (TIMP-1) and matrix metalloproteinase 13 (MMP-13) in human umbilical vein endothelial cells induced by transforming growth factor-β. ALK5-IN-82 shows potential for use in research related to cardiac fibrosis.

Fluoxetine-Conjugated Platinum(IV) prodrug-1 is an eEF2K inhibitor that can hinder the proliferation of cancer cells, induce DNA damage, and cause cell cycle arrest at the S phase, leading to apoptosis (Apoptosis). It also promotes the accumulation of reactive oxygen species (ROS) and disrupts mitochondrial function. This prodrug inhibits the migration and invasion of TNBC cells by suppressing MMP-2 activity and induces autophagy in TNBC cells through AMPK activation. In the 4T1-Luc mouse model, it exhibits antitumor activity and triggers immune suppression. Fluoxetine-Conjugated Platinum(IV) prodrug-1 is relevant for research in triple-negative breast cancer (TNBC).

MMP-11-IN-1 is a new class of phosphinate prodrugs. It is the glycosyl ester of RXP03 and can enhance blood-brain barrier (BBB) permeability.

MMP-9/10-IN-1 (Compound 6b) is a potent dual inhibitor of MMP-9/10, with IC50 values of 0.076 μM for NSCLC cells and 0.139 μM for A549 cells. When combined with Sorafenib, it exhibits anti-invasive and anti-angiogenic properties.

Linvemastat (Compound FC-4) is an orally active MMP-12 inhibitor with an IC50 of less than 10 nM and demonstrates high selectivity over MMP-1, -2, -3, -7, -9, -10, and -14. It significantly reduces lung fibrosis in a mouse model of bleomycin-induced unilateral pulmonary fibrosis and effectively alleviates kidney damage, interstitial inflammation, or fibrosis in a unilateral ureteral obstruction renal fibrosis model. Linvemastat is suitable for research into inflammatory diseases such as idiopathic pulmonary fibrosis (IPF), inflammatory bowel disease (IBD), and asthma.

Cystatin Bagonist 1 is an orally active inhibitor of MMP-2/9. It suppresses U87 and T98G cells with IC50 values of 3.95 μM and 3.43 μM, respectively. Cystatin Bagonist 1 induces S-phase cell cycle arrest in MG cells and inhibits their angiogenesis, migration, and invasion. Additionally, it hinders tumor growth in U87 MG xenograft models. This compound is applicable for research in malignant glioma (MG).

BRK/PTK6-IN-1 (Compound 51) is a potent and selective BRK inhibitor with an IC50 of 3.37 nM and Kd of 44 nM. It reduces MMP-9 protein expression and inhibits IGF-1-induced AKT phosphorylation in MDA-MB-231 cells. This compound significantly hinders migration, invasion, and colony formation without affecting cell proliferation and is commonly used in breast cancer and other cancer research.

14-3-3-IN-2 is an inhibitor of the 14-3-3 protein, exhibiting an IC50 value of 15 nM. It disrupts the interaction between 14-3-3α and aminopeptidase N, while also downregulating the mRNA levels of matrix metalloproteinase-1 (MMP-1) that are elevated by 14-3-3α.

NSD2/H3K36me2 modulator-1 is an orally active modulator targeting NSD2/H3K36me2. It competitively binds to the SAM pocket of NSD2, effectively inhibiting NSD2 expression and H3K36me2 methylation. This compound can also reverse epithelial-mesenchymal transition (EMT), inhibit cell migration, and induce G0/G1 phase arrest and apoptosis (apoptosis). Additionally, NSD2/H3K36me2 modulator-1 reduces mitochondrial membrane potential (MMP) and promotes reactive oxygen species (ROS) generation. It is used in research for developing epigenetic anticancer strategies targeting NSD2 in hepatocellular carcinoma (HCC).

Multi-kinase-IN-8 is a multi-kinase inhibitor. It effectively inhibits COX-1 (IC50 = 12.6 μM), COX-2 (IC50 = 0.05 μM), and VEGFR-2 (IC50 = 0.12 nM). Additionally, it blocks tumor-associated carbonic anhydrases CA IX and CA XII with Ki values of 31.5 nM and 386.9 nM, respectively, and induces cell cycle arrest and apoptosis (apoptosis) by upregulating Caspase-9 and Bax, while downregulating Bcl-2. Multi-kinase-IN-8 also suppresses the expression of PGE2, p-VEGFR-2, MMP-9, and HIF-1α, and demonstrates growth inhibitory activity on breast, lung, and colorectal adenocarcinomas.

MMP-2/MMP-9-IN-1 is a potent, highly selective, and orally bioavailable inhibitor of type IV collagenases [MMP-9 and MMP-2], exhibiting IC50 values of 0.24 μM for MMP-9 and 0.31 μM for MMP-2, which can be used to study cancer.

MMP-9-IN-13 (Example 1) is a selective human MMP-9 inhibitor with an IC50 value of 0.02 nM, applicable for studies related to the ocular surface.

ONO-4817 is a broad-spectrum matrix metalloproteinase (MMP) inhibitor that potentially mitigates atherosclerotic neointimal proliferation and atheromatous plaque progression by suppressing matrix metalloproteinases (MMPs). It effectively reduces the development of aortic intimal hyperplasia in experimental hyperlipidemic rabbits [1].

Broad spectrum MMP inhibitor (IC₅₀ values are 0.7, 0.9, 13, 16 and 1170 nM for MMP-2, MMP-13, MMP-9, MMP-3 and MMP-1 respectively). Attenuates early left ventricular dilation after experimental myocardial infarction in mice.

RS-104966 is an inhibitor of collagenase that acts by inducing the conformational change in the side-chains of the S1 pocket of MMP-1.