mmp13 in 2

MMP13-IN-2 is a highly potent, selective, and orally active inhibitor of MMP-13. It demonstrates exceptional potency against MMP-13, with an IC50 value of 0.036 nM, and exhibits selectivities greater than 1,500-fold over MMP-1, 3, 7, 8, 9, 14, and TACE. Moreover, MMP13-IN-2 possesses the capability to effectively inhibit collagen release from cartilage in vitro. Consequently, MMP13-IN-2 holds great potential for advancing research on collagenase-related diseases.

Acetamide, N-[2-[(5-chloro-2 methoxyphenyl)amino]-4'-methyl[4,5'-bithiazol]-2'-yl]-inhibits pro-matrix metalloproteinase activation and can be used to prevent, treat or ameliorate MMP9 and or MMP13-mediated syndromes.

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.

Highly potent and selective MMP13 inhibitor (IC50 = 6.9 pM). Exhibits >2600-fold selectivity for MMP13 over related MMPs. Inhibits degradation of bovine nasal septum cartilage explants in vitro . Orally bioavailable. Nara et al (2014) Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1 binding site. Bioorg.Med.Chem. 22 5487 PMID:25192810

MMP13-IN-5 (compound 13m) is a potent and selective inhibitor of MMP-2 and MMP-13, with IC50 values of 3.6 μM for MMP-2 and 14.6 μM for MMP-13, implicated in osteoarthritis (OA) pathology [1].