mmp14

CTS-1027 is a small molecule inhibitor of MMPs (IC50s: 0.3 nM, 0.5 nM for MMP2, MMP13). It has > 1,000 fold selectivity over MMP1.

Marimastat (BB2516) (BB-2516) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor. MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM)and MMP-7 (IC50=13 nM).

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

UK-370106 is a potent and highly selective inhibitor of MMP-3 (IC50: 23 nM) and MMP-12 (IC50: 42 nM), effectively inhibiting the cleavage of [3H]-fibronectin by MMP-3 (IC50: 320 nM).

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.

UK 356618 is a potent and selective inhibitor of matrix metalloprotease-3 (IC50: 5.9 nM).

BPHA (MMP-2/MMP-9 Inhibitor II) is a potent, selective and orally active inhibitor of MMP-2, MMP-9 and MMP-14 with IC50s of 12 nM, 16 nM and 17 nM, respectively.BPHA does not inhibit MMP-1, -3 and -7 (IC50s of 974, >1000 and 795 nM, respectively).BPHA has anti-angiogenic and BPHA has anti-angiogenic and anti-tumor activities.

JG26 is a potent inhibitor of ADAM17, which can inhibit ADAM8, ADAM17, ADAM10 and MMP-12, with IC50 values of 12 nM, 1.9 nM, 150 nM and 9.4 nM, respectively, and can be used to study the immune system of the body.

CP-544439 is an orally active and potent MMP-13 inhibitor that prevents diet-induced obesity and inhibits adipogenesis in 3T3-L1 preadipocytes in mice, and can be used for the study of obesity.

3-Aminobenzene-1,2-diol (compound C8) is an inhibitor of matrix metalloproteinases (MMP), with IC50 values of 20, 26, 16, and 16.3 μM against MMP-2, MMP-8, MMP-9, and MMP-14, respectively.

ND-336 is a highly selective inhibitor ofMMP-2, MMP-9 and MMP-14. ND-336 accelerates diabetic wound healing by lowering inflammation and by enhancing angiogenesis and re-epithelialization of the wound.

TMI-1 (WAY-171318), a novel orally active inhibitor of ADAM17 (TACE) and MMP, induces tumor apoptosis in a breast cancer.

Aldumastat (GLPG1972) is a highly potent, specific and orally active inhibitor of ADAMTS-5.Aldumastat is used for the study of osteoarthritis of the knee.

CMC2.24 (TRB-N0224) is an orally active tricarbonylmethane agent that demonstrates effectiveness in inhibiting Ras activation and the downstream effector ERK1/2 pathway, thus effectively combating pancreatic tumor formation in mice. Additionally, CMC2.24 exerts potent inhibitory effects on zinc-dependent MMPs, with IC50s ranging from 2.0-69 μM. Furthermore, CMC2.24 aids in alleviating the progression of osteoarthritis by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis through the NF-κB/HIF-2α axis[1][2][3].

(R)-ND-336 is a highly potent and selective MMP-9 inhibitor with a K_i value of 19 nM and also exhibits inhibitory activity against MMP-2 (K_i = 127 nM) and MMP-14 (K_i = 119 nM). With significant potential, (R)-ND-336 is being investigated in diabetic foot ulcers (DFUs) research [1].

KP-457 is a specific inhibitor of a disintegrin-metalloproteinase 17 (ADAM17) and a TNFα converting enzyme TACE inhibitor that blocks the production of soluble TNF (sTNF).

MMP-7-IN-2 acts as a selective and potent MMP7 inhibitor and can be used to study inflammatory responses and vascular-related diseases.

N-Acetylgalactosaminyltransferase 1 (GALNT1) is a glycosyltransferase that initiates mucin-type O-glycosylation by transferring α-GalNAc from UDP-GalNAc to serine (Ser) or threonine (Thr) residues in proteins. Overexpression of N-Acetylgalactosaminyltransferase 1 in gastric cancer enhances the aberrant O-glycosylation of CD44, activating the Wnt/β-catenin signaling pathway and influencing the malignant behavior of gastric cancer cells. This enzyme plays a crucial role in cancer progression and metastasis by modifying the O-glycosylation of various glycoproteins such as mucin (MUC1), osteopontin (OPN), matrix metalloproteinase-14 (MMP14), and integrin α3.