DGK-θ Activators
DGK-θ activators encompass a spectrum of biochemical agents that enhance the activity of diacylglycerol kinase theta (DGK-θ), each utilizing distinct pathways to exert their effects. Molecules like Phorbol 12-myristate 13-acetate (PMA) function as diacylglycerol (DAG) mimetics, activating protein kinase C (PKC), which in turn promotes DGK-θ activity to regulate DAG levels within a feedback mechanism. Ceramide and Sphingosine-1-phosphate (S1P) act through different routes; ceramide activates protein phosphatase 2A (PP2A), which modulates DGK-θ, while S1P engages G-protein coupled receptors (S1PRs), triggering downstream effects that lead to DGK-θ activation.
Other activators operate indirectly; for instance, arachidonic acid is metabolized into eicosanoids that influence signaling pathways affecting DGK-θ activity. Compounds like bryostatin-1 and the synthetic alkyl-lysophospholipid edelfosine target PKC isoforms, which are integral to the regulatory network controlling DAG and phosphatidic acid balance, thereby modulating DGK-θ. These activators not only play pivotal roles in the complex lipid signaling network but also contribute to maintaining cellular lipid homeostasis.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
PMA | 16561-29-8 | sc-3576 sc-3576A sc-3576B sc-3576C sc-3576D | 1 mg 5 mg 10 mg 25 mg 100 mg | $41.00 $132.00 $214.00 $500.00 $948.00 | 119 | |
PMA acts as a diacylglycerol (DAG) analog, directly activating protein kinase C (PKC). DGK-θ regulates intracellular levels of DAG by phosphorylating DAG to produce phosphatidic acid. PMA-induced PKC activation can enhance DGK-θ activity as part of a feedback mechanism to control DAG levels. | ||||||
C2 Ceramide | 3102-57-6 | sc-201375 sc-201375A | 5 mg 25 mg | $124.00 $460.00 | 12 | |
Ceramide can activate protein phosphatase 2A (PP2A), which in turn dephosphorylates and activates DGK-θ, leading to increased DGK-θ activity and a subsequent decrease in DAG concentrations. | ||||||
D-erythro-Sphingosine-1-phosphate | 26993-30-6 | sc-201383 sc-201383D sc-201383A sc-201383B sc-201383C | 1 mg 2 mg 5 mg 10 mg 25 mg | $165.00 $322.00 $570.00 $907.00 $1727.00 | 7 | |
S1P binds to its G-protein coupled receptors (S1PRs), which can lead to the activation of DGK-θ through downstream signaling pathways, thereby reducing DAG levels and promoting the synthesis of phosphatidic acid. | ||||||
Arachidonic Acid (20:4, n-6) | 506-32-1 | sc-200770 sc-200770A sc-200770B | 100 mg 1 g 25 g | $92.00 $240.00 $4328.00 | 9 | |
Arachidonic acid can be released by phospholipase A2 and serve as a precursor for eicosanoids, which can activate signaling pathways that indirectly enhance DGK-θ activity to regulate DAG levels within cells. | ||||||
Bryostatin 1 | 83314-01-6 | sc-201407 | 10 µg | $245.00 | 9 | |
Bryostatin-1 acts as a PKC modulator. It can activate specific PKC isoforms which can then enhance DGK-θ activity as part of the signaling cascade that regulates DAG and phosphatidic acid homeostasis. | ||||||
1,2-Dioctanoyl-sn-glycerol | 60514-48-9 | sc-202397 sc-202397A | 10 mg 50 mg | $47.00 $254.00 | 2 | |
Although DAG directly activates PKC, it is also the substrate for DGK-θ. An increase in DAG levels can enhance DGK-θ activity as the enzyme works to convert excess DAG to phosphatidic acid, thus maintaining cellular homeostasis. | ||||||
Lithium | 7439-93-2 | sc-252954 | 50 g | $214.00 | ||
Lithium can inhibit inositol monophosphatase, leading to reduced levels of IP3 and DAG. This may indirectly enhance DGK-θ activity as part of a compensatory mechanism to balance the reduced DAG levels. | ||||||
Retinoic Acid, all trans | 302-79-4 | sc-200898 sc-200898A sc-200898B sc-200898C | 500 mg 5 g 10 g 100 g | $66.00 $325.00 $587.00 $1018.00 | 28 | |
Retinoic acid influences various signaling pathways and can increase the expression of certain PKC isoforms. This may lead to enhanced DGK-θ activity through PKC-mediated regulatory mechanisms. | ||||||
Dexamethasone | 50-02-2 | sc-29059 sc-29059B sc-29059A | 100 mg 1 g 5 g | $91.00 $139.00 $374.00 | 36 | |
Dexamethasone can induce the expression of certain isoforms of PKC, which may indirectly enhance DGK-θ activity by modulating the pathways that control DAG and phosphatidic acid levels. | ||||||
A23187 | 52665-69-7 | sc-3591 sc-3591B sc-3591A sc-3591C | 1 mg 5 mg 10 mg 25 mg | $55.00 $131.00 $203.00 $317.00 | 23 | |
A23187 acts as an ionophore that increases intracellular calcium levels, potentially activating calcium-sensitive PKC isoforms and thereby indirectly enhancing DGK-θ activity. | ||||||