ADAM39 Inhibitors
ADAM39 inhibitors are a class of chemical compounds designed to specifically inhibit the activity of ADAM39, a member of the ADAM (A Disintegrin And Metalloprotease) family of proteins. ADAM39, like other ADAM family members, contains both metalloprotease and disintegrin domains, which play a role in protein cleavage and cell-cell or cell-matrix adhesion, respectively. The metalloprotease domain is responsible for catalyzing the proteolytic cleavage of peptide bonds in substrates, a process involved in many biological activities such as protein shedding, signaling, and extracellular matrix remodeling. ADAM39 inhibitors are developed to block the enzyme's proteolytic function by binding to its active site or key regulatory regions, thus preventing substrate cleavage. These inhibitors typically contain chemical groups such as hydroxamates, thiols, or carboxylates that coordinate with the zinc ion present in the enzyme's active site, effectively neutralizing the enzyme's catalytic activity.
The structural design of ADAM39 inhibitors is informed by detailed studies of the enzyme's three-dimensional conformation, usually determined through methods like X-ray crystallography or cryo-electron microscopy. These structural insights reveal the key features of the metalloprotease active site, including the arrangement of catalytic residues and the zinc ion that is crucial for enzymatic activity. Based on this information, researchers can design inhibitors that specifically bind to these regions, ensuring high specificity for ADAM39 while avoiding off-target effects on related metalloproteases. In addition to direct binding to the active site, some ADAM39 inhibitors may function allosterically, binding to regions outside of the catalytic domain and inducing conformational changes that impair the enzyme's function. Computational techniques such as molecular docking and dynamic simulations are frequently used to predict and optimize the interactions between ADAM39 and its inhibitors, improving binding affinity and selectivity. By inhibiting ADAM39, researchers can explore its role in processes like extracellular matrix remodeling, cell adhesion, and proteolytic regulation, offering valuable insights into the biological pathways that rely on this metalloprotease.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Marimastat | 154039-60-8 | sc-202223 sc-202223A sc-202223B sc-202223C sc-202223E | 5 mg 10 mg 25 mg 50 mg 400 mg | $165.00 $214.00 $396.00 $617.00 $4804.00 | 19 | |
Marimastat is a broad-spectrum matrix metalloprotease inhibitor that would inhibit a disintegrin and metallopeptidase domain 39 (ADAM39) by binding to its catalytic zinc ion, directly preventing the proteolytic cleavage of peptide bonds in substrates. | ||||||
Batimastat | 130370-60-4 | sc-203833 sc-203833A | 1 mg 10 mg | $175.00 $370.00 | 24 | |
Batimastat, a synthetic inhibitor, directly binds to the active site of ADAM39, blocking its ability to interact with and process its substrates, leading to the inhibition of the protein's enzymatic function. | ||||||
GM 6001 | 142880-36-2 | sc-203979 sc-203979A | 1 mg 5 mg | $75.00 $265.00 | 55 | |
GM6001, also known as Galardin, is a broad-spectrum matrix metalloproteinase inhibitor that would inhibit ADAM39 by binding to its active site, preventing the proteolytic action of the enzyme on its specific substrates. | ||||||
PD 168393 | 194423-15-9 | sc-222138 | 1 mg | $162.00 | 4 | |
PD 166793 is designed to inhibit the metalloproteinase activity of collagenases and stromelysins, which are structurally related to ADAM39; it would inhibit ADAM39 by occupying the enzymatic pocket, obstructing substrate access and catalysis. | ||||||
WAY 170523 | 307002-73-9 | sc-361402 sc-361402A | 1 mg 10 mg | $275.00 $595.00 | 1 | |
WAY-170523 is an inhibitor of MMP-13, a matrix metalloproteinase with similar active site characteristics to ADAM39; it would inhibit ADAM39 by binding to the active site and preventing the interaction with substrate proteins, thereby inhibiting the proteolytic activity of the enzyme. | ||||||
Prinomastat | 192329-42-3 | sc-507449 | 5 mg | $190.00 | ||
Prinomastat is a matrix metalloproteinase inhibitor that can inhibit ADAM39 by mimicking substrate structure, competitively binding to the enzyme's active site, and preventing the normal substrate processing. | ||||||
Ro 32-3555 | 190648-49-8 | sc-296277 | 10 mg | $413.00 | 2 | |
Ro 32-3555 is an inhibitor of metalloproteinases that would inhibit ADAM39 by selectively associating with its metalloprotease domain, thereby inhibiting the proteolytic function essential to the protein's activity in the cell. | ||||||
Andrographolide | 5508-58-7 | sc-205594 sc-205594A | 50 mg 100 mg | $15.00 $39.00 | 7 | |
Andrographolide inhibits NF-kB activation; since NF-kB can regulate the expression of various ADAMs, consistent inhibition of NF-kB by Andrographolide could decrease the functional activity of ADAM39 by reducing the expression of proteins that might be substrates or modulators of ADAM39, leading to a decrease in its functional proteolytic activity without affecting the expression levels of ADAM39 itself. | ||||||
Doxycycline-d6 | 564-25-0 unlabeled | sc-218274 | 1 mg | $16500.00 | ||
Doxycycline, while primarily an antibiotic, also serves as a non-selective inhibitor of matrix metalloproteinases and would inhibit ADAM39 by binding to the metalloenzyme active site, thereby blocking the cleavage of substrates. | ||||||
SB-3CT | 292605-14-2 | sc-205847 sc-205847A | 1 mg 5 mg | $100.00 $380.00 | 15 | |
SB-3CT is a selective inhibitor of gelatinases; by analogy, it could inhibit ADAM39 by targeting the gelatinase-like domain present in the protein, inhibiting the proteolytic activity that is central to the protein's function. | ||||||