MMP-10 Inhibitor

BI-4394 (MMP13-IN-3), a chemical probe, is a potent, selective, and orally active MMP-13 inhibitor (IC₅₀=1 nM) for the potential treatment of osteoarthritis. BI-4394 is >1000 selective over other MMPs.

MMP-9/10-IN-2 (compound 6e) is a potent inhibitor of MMP10 and MMP9, with IC₅₀ of 0.076 μM for MMP10, and 93.18% inhibition at 0.5 μM for MMP9. MMP-9/10-IN-2 plays an important role in anti-tumor.

Snail IN-1 is an orally active Snail inhibitor with a Ka of 0.36 μM.Snail IN-1 disrupts Snail-CBP interaction, accelerates Snail protein degradation, reduces Snail acetylation, increases Snail polyubiquitination, and selectively downregulates Snail protein without altering other EMT transcription factors.Snail IN-1 reduces atherosclerotic plaque burden, modulates inflammation and plaque stability factors, downregulates CCL5, CXCL10, MMP2, and MMP9, and upregulates α-smooth muscle actin.Snail IN-1 exerts anti-inflammatory and plaque-stabilizing properties.Snail IN-1 can be used for the research of atherosclerosis.

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.

CM-352 (compound 5) is an inhibitor of matrix metalloproteinases (MMPs) (MMP-3: IC₅₀=15 nM; MMP-10: IC₅₀=12 nM). CM-352 has significant antifibrinolytic activity (EC₅₀=0.7 nM) and can significantly prolong blood coagulation time. CM-352 can be used in anti-bleeding research.