nPKC θ Inhibitors
nPKC θ (novel protein kinase C theta) inhibitors represent a class of chemical compounds that are designed to selectively target and inhibit the activity of the protein kinase C theta isoform. Protein kinase C (PKC) enzymes are a family of serine/threonine kinases that play pivotal roles in cell signaling and regulation. Among the various isoforms of PKC, nPKC θ is distinctive for its specific involvement in immune responses and inflammation. As a result, the development of nPKC θ inhibitors has garnered significant attention in the field of molecular pharmacology and drug discovery.
These inhibitors are characterized by their ability to interact with the active site of nPKC θ and impede its enzymatic function. This inhibition can occur through various mechanisms, including competitive binding to the ATP-binding site, allosteric regulation, or interference with the kinase's substrate recognition. The rationale behind targeting nPKC θ lies in its significant role in immune cell activation, particularly in T lymphocytes. By selectively inhibiting this isoform, researchers aim to modulate immune responses without affecting other PKC isoforms, which have distinct functions in various cellular processes. The development of nPKC θ inhibitors holds promise for a range of potential applications, especially in the context of autoimmune diseases, inflammatory disorders, and cancer, where immune system dysregulation plays a significant role.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Sotrastaurin | 425637-18-9 | sc-474229 sc-474229A | 5 mg 10 mg | $300.00 $540.00 | ||
Sotrastaurin is a pan-PKC inhibitor, which means it inhibits multiple isoforms of PKC. Its inhibition is based on competing with ATP for binding to the catalytic domain of PKC. Given that nPKCθ is a member of the PKC family, Sotrastaurin can inhibit nPKCθ by blocking its ATP-binding site. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $103.00 $237.00 | 36 | |
It's a commonly used ATP-competitive inhibitor of PKC. By competing with ATP for the kinase's catalytic site, BIM prevents the phosphorylation activity of various PKC isoforms, including nPKCθ. | ||||||
Gö 6983 | 133053-19-7 | sc-203432 sc-203432A sc-203432B | 1 mg 5 mg 10 mg | $103.00 $293.00 $465.00 | 15 | |
A broad-spectrum PKC inhibitor. It affects various PKC isoforms by competing with ATP for binding, hence preventing the kinase from transferring phosphate groups to its substrates. | ||||||
Gö 6976 | 136194-77-9 | sc-221684 | 500 µg | $223.00 | 8 | |
Although it's known primarily as a cPKC inhibitor, its mechanism involves ATP-competitive inhibition, which can also affect nPKCθ. | ||||||
Rottlerin | 82-08-6 | sc-3550 sc-3550B sc-3550A sc-3550C sc-3550D sc-3550E | 10 mg 25 mg 50 mg 1 g 5 g 20 g | $82.00 $163.00 $296.00 $2050.00 $5110.00 $16330.00 | 51 | |
Historically thought to be a specific inhibitor of PKC-delta, the exact mechanism of Rottlerin's inhibition is still under debate. It's considered to be an ATP-competitive inhibitor, but it may also disrupt the PKC conformation or its interaction with substrates. | ||||||
Enzastaurin | 170364-57-5 | sc-364488 sc-364488A sc-364488B | 10 mg 50 mg 200 mg | $254.00 $600.00 $1687.00 | 3 | |
Primarily a PKCβ inhibitor, Enzastaurin also acts in an ATP-competitive manner. Although its main target is PKCβ, its broad action on PKC isoforms means it can also inhibit nPKCθ. | ||||||
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $150.00 $388.00 | 113 | |
A potent, non-selective kinase inhibitor. Staurosporine has a broad range of kinase targets because it can effectively compete with ATP for binding to the kinase's catalytic site. Its potent inhibition of PKC isoforms, including nPKCθ, comes from this ATP-competitive action. | ||||||
Chelerythrine | 34316-15-9 | sc-507380 | 100 mg | $540.00 | ||
Derived from plants, chelerythrine acts as a PKC inhibitor by intercalating into the ATP-binding pocket of the kinase. This prevents ATP from binding and subsequently inhibits the phosphorylation activity of PKC isoforms, including nPKCθ. | ||||||