DGK-θ Inhibitors
Chemical inhibitors of DGK-θ include a variety of compounds that target the enzyme's activity through different mechanisms. R59949 and R59022 are direct inhibitors of DGK-θ, functioning by obstructing the phosphorylation of diacylglycerol (DAG) to phosphatidic acid (PA). This blockage leads to an accumulation of DAG, a substrate for DGK-θ, thereby preventing the conversion to PA and functionally inhibiting the activity of DGK-θ. Similarly, CID755673 competes with ATP for binding to DGK-θ, which is critical for the enzyme's activity in phosphorylating DAG. By preventing ATP binding, CID755673 effectively hinders the enzymatic function of DGK-θ.
Furthermore, several inhibitors act on DGK-θ through its regulatory pathways. Calphostin C, Gö 6983, Staurosporine, Sotrastaurin, Bisindolylmaleimide I, and Ritanserin inhibit protein kinase C (PKC), an upstream activator of DGK-θ. By inhibiting PKC, these compounds indirectly reduce the phosphorylation and activation of DGK-θ, leading to a decrease in its functional activity. The inhibition of PKC prevents it from phosphorylating and activating DGK-θ, thereby diminishing the enzyme's ability to convert DAG to PA. D609, while known as a phosphatidylcholine-specific phospholipase C inhibitor, also impinges on DGK-θ activity. It alters lipid signaling pathways that are integral to the function of DGK-θ, thereby achieving an indirect functional inhibition of the protein.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
R 59-022 | 93076-89-2 | sc-203227 | 5 mg | $124.00 | 1 | |
R59022 is another DGK inhibitor that operates in a manner similar to R59949. It directly inhibits DGK-θ by obstructing the enzymatic conversion of DAG to PA, leading to the functional inhibition of the protein by maintaining high levels of DAG and low levels of PA within the cell. | ||||||
Calphostin C | 121263-19-2 | sc-3545 sc-3545A | 100 µg 1 mg | $343.00 $1642.00 | 20 | |
Calphostin C is a potent inhibitor of protein kinase C (PKC). Since PKC is one of the upstream activators of DGK-θ, which can phosphorylate and activate DGK-θ, Calphostin C inhibits DGK-θ activity indirectly by inhibiting PKC, which is necessary for DGK-θ activation. | ||||||
Gö 6983 | 133053-19-7 | sc-203432 sc-203432A sc-203432B | 1 mg 5 mg 10 mg | $105.00 $299.00 $474.00 | 15 | |
Gö 6983 is a broad-spectrum PKC inhibitor. By inhibiting PKC, it indirectly inhibits the activation of DGK-θ, as PKC can phosphorylate and activate DGK-θ. This decreases the functional activity of DGK-θ by preventing its activation. | ||||||
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $153.00 $396.00 | 113 | |
Staurosporine is a non-selective kinase inhibitor known to inhibit a wide range of protein kinases. By inhibiting upstream kinases that contribute to DGK-θ activation, such as PKC, staurosporine indirectly reduces the functional activity of DGK-θ. | ||||||
Sotrastaurin | 425637-18-9 | sc-474229 sc-474229A | 5 mg 10 mg | $300.00 $540.00 | ||
Sotrastaurin is a selective PKC inhibitor. It inhibits DGK-θ indirectly by preventing PKC-mediated phosphorylation and subsequent activation of DGK-θ, leading to reduced functional activity of DGK-θ. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $105.00 $242.00 | 36 | |
Bisindolylmaleimide I is a specific inhibitor of PKC. By inhibiting PKC, it can indirectly inhibit the functional activity of DGK-θ by preventing its necessary phosphorylation and activation by PKC. | ||||||
D609 | 83373-60-8 | sc-201403 sc-201403A | 5 mg 25 mg | $189.00 $575.00 | 7 | |
D609 is a phosphatidylcholine-specific phospholipase C inhibitor, but it also inhibits DGK activity. It indirectly inhibits DGK-θ by altering lipid signaling pathways that are necessary for DGK-θ function, leading to functional inhibition of the protein. | ||||||
Ritanserin | 87051-43-2 | sc-203681 sc-203681A | 10 mg 50 mg | $89.00 $312.00 | 2 | |
Ritanserin is primarily a serotonin receptor antagonist, but it has been shown to inhibit PKC as well. By inhibiting PKC, it indirectly inhibits DGK-θ through the downregulation of PKC-mediated activation pathways, leading to reduced activity of DGK-θ. | ||||||