MMP-1 Inhibitor

Hydrangenol is an orally active antiphotoaging compound. It can be isolated from Hydrangea serrata leaves. Hydrangenol prevents wrinkle formation by reducing MMP and inflammatory cytokine expression and increasing moisturizing factors and antioxidant genes level.

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.

Prinomastat hydrochloride (AG3340 hydrochloride) 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 hydrochloride 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 hydrochloride can cross blood-brain barrier. Antitumor avtivity.

Cipemastat is a potent, competitive inhibitor of human collagenases 1, 2 and 3 with K_is of 3.0, 4.4 and 3.4 nM, respectively.

CP-471474 is an orally active and pan MMP inhibitor, with IC₅₀ values of 1170 nM (MMP-1), 0.7 nM (MMP-2), 16 nM (MMP-3), 13 nM (MMP-9) and 0.9 nM (MMP-13), respectively.

MMP3 inhibitor 1 is a potent and highly selective MMP-3 inhibitor with an IC₅₀ of 1 nM.

XL-784 is a selective matrix metalloproteinases (MMP) inhibitor, with IC₅₀s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1, MMP-2, MMP-3, MMP-8, MMP-9, MMP-13, respectively.

CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC₅₀s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis.

BPHA is a potent and orally active MMP-2, MMP-9 and MMP-14 inhibitor with IC₅₀s of 12 nM, 16 nM and 17 nM, respectively. BPHA does not inhibit MMP-1, -3, and -7 (the IC₅₀s are 974, >1000, and 795 nM, respectively). BPHA has antiangiogenic and antitumor effects.

Linvemastat (Compound FC-4) is an orally active MMP-12 inhibitor (IC₅₀: < 10  nM) with high selectivity of MMP-1, -2, -3, -7, -9, -10 and -14. Linvemastat significantly attenuates lung fibrosis in Bleomycin (HY-108345) induced unilateral lung fibrosis mice model and potently reduces kidney damage, interstitial inflammation or fibrosis in kidney fibrosis model of unilateral ureteral occlusion. Linvemastat can be used for inflammatory diseases research, such as idiopathie pulmonary fibrosis (IPF), inflammatory bowel disease (IBD) and asthma.

14-3-3-IN-2 is a 14-3-3 protein inhibitor with an IC₅₀ of 15 nM. 14-3-3-IN-2 can disrupt the interaction of 14-3-3α with aminopeptidase N and down-regulate 14-3-3α increased MMP-1 mRNA levels.

MMP-2 Inhibitor II (compound 2) is a selective MMP-2 inhibitor. The Kinetic parameters for MMP inhibition are 2.4 μM (MMP-2), 45 μM (MMP-1), and 379 μM (MMP-7), respectively.

RS-104966 is a potent collagenase-1 (MMP-1) inhibitor. RS-104966 induces a conformational change in the side chains of the S10 pocket of MMP-1.

Ethyl trans-caffeate is a matrix metalloproteinase inhibitor (MMP-1, MMP-2, MMP-9). Ethyl trans-caffeate can be isolated from Artemisia aucheri. Ethyl trans-caffeate binds to the SARS-CoV-2 main protease by forming a hydrogen bond with Thr190. The PMK extract of Pandanus tectorius fruit containing Ethyl trans-caffeate inhibits HMG-CoA reductase activity. Ethyl trans-caffeate can be used in research on COVID-19 and atherosclerosis.

RP 59794 is a potent collagenase (collagenase) and broad-spectrum matrix metalloproteinase (MMP) inhibitor. The active stereoisomer of RP 59794 has a K_i of 13 nM against MMP-1 (with native collagen as substrate) and 45 nM (with a synthetic octapeptide as substrate). RP 59794 blocks and partially dissociates TIMP by binding to the active site of collagenase, specifically inhibits the collagen-transmigrating migration of osteoclasts and bone resorption on collagen-coated surfaces, but exerts no effect on cell migration in collagen-free environments, and acts in a time-dependent manner in bone tissues. RP 59794 can be used in studies of arthritis, periodontal disease, corneal ulcers and tumor invasion.

CGS 27023A free base is a non-peptidic and orally active MMP inhibitor with the K_i values of 43, 33, 20 and 8 nM for MMP-3, MMP-1, MMP-2 amd MMP-9, respectively. CGS 27023A free base prevents cartilage degradation in stromelysin-induced rabbit cartilage degradation model. CGS 27023A free base can be used for study of arthritis.

MMP-9-IN-5 is a MMP-9 inhibitor (IC₅₀: 4.49 nM) that forms hydrogen bond with MMP-9. MMP-9-IN-5 also inhibits _AKT activity (IC₅₀: 1.34 nM). MMP-9-IN-5 shows cell cytotoxicity and induces cell apoptosis. MMP-9-IN-5 can be used in the research of cancers.

CP-544439 is a potent and orally active matrix metalloproteinase-13 (MMP-13) inhibitor with an IC₅₀ of 0.75 nM.

CGS 27023A is a non-peptidic and orally active MMP inhibitor with the K_i values of 43, 33, 20 and 8 nM for MMP-3, MMP-1, MMP-2 amd MMP-9, respectively. CGS 27023A prevents cartilage degradation in stromelysin-induced rabbit cartilage degradation model. CGS 27023A can be used for study of arthritis.

MMP-9-IN-4 is a MMP-9 inhibitor (IC₅₀: 7.46 nM) that has H-π interactions with MMP-9. MMP-9-IN-4 also inhibits _AKT activity (IC₅₀: 8.82 nM). MMP-9-IN-4 shows cell cytotoxicity and induces cell apoptosis. MMP-9-IN-4 can be used in the research of cancers.