THEG Activators
THEG can be grouped based on their primary mechanisms of action, mainly focusing on the elevation of intracellular cyclic AMP (cAMP) levels or the activation of specific protein kinases that may regulate THEG activity. Forskolin, Isoproterenol, PGE1 (Prostaglandin E1), BAY 60-6583, and Rolipram are representatives that primarily augment cAMP levels within cells. Forskolin directly stimulates adenylyl cyclase, thereby increasing cAMP production. Isoproterenol, a beta-adrenergic agonist, and PGE1 activate cAMP synthesis via their respective G protein-coupled receptors. BAY 60-6583, through its selective action on adenosine A2B receptors, also promotes cAMP accumulation. Rolipram achieves a similar result by inhibiting phosphodiesterase 4, preventing cAMP breakdown. Together, these agents raise cAMP levels, which can activate THEG, assuming that THEG's function is modulated by cAMP-dependent pathways, such as those mediated by protein kinase A (PKA).
Other chemicals operate through distinct kinase pathways or by modulating cAMP-related processes. Anisomycin activates stress-activated protein kinases, which could phosphorylate and activate THEG if it is part of the stress response mechanism. PMA, a known activator of protein kinase C (PKC), could also phosphorylate THEG if THEG is regulated by PKC-associated pathways. IBMX and Cilostazol both prevent the degradation of cAMP, IBMX by non-specific inhibition of phosphodiesterases and Cilostazol by specifically inhibiting phosphodiesterase 3. The resulting elevation in cAMP can lead to PKA activation, which in turn may activate THEG. Additionally, Vardenafil and Sildenafil, both phosphodiesterase 5 inhibitors, primarily increase cGMP levels, but the subsequent increase in cAMP through cross-activation of signaling pathways could also influence THEG activity. Zaprinast, by inhibiting phosphodiesterase 5, can lead to increased levels of both cAMP and cGMP, possibly affecting THEG if its activity is regulated by cyclic nucleotide signaling.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Isoproterenol Hydrochloride | 51-30-9 | sc-202188 sc-202188A | 100 mg 500 mg | $28.00 $38.00 | 5 | |
Isoproterenol is a beta-adrenergic agonist that stimulates adenylyl cyclase via G protein-coupled receptor activation, increasing cAMP levels which could activate THEG through downstream PKA activation if THEG is regulated by this pathway. | ||||||
PGE1 (Prostaglandin E1) | 745-65-3 | sc-201223 sc-201223A | 1 mg 10 mg | $31.00 $145.00 | 16 | |
Prostaglandin E1 binds to its G-protein-coupled receptor, leading to an increase in cAMP production. This elevation in cAMP may result in activation of THEG if it is responsive to changes in cAMP levels or downstream PKA signaling. | ||||||
IBMX | 28822-58-4 | sc-201188 sc-201188B sc-201188A | 200 mg 500 mg 1 g | $260.00 $350.00 $500.00 | 34 | |
IBMX is a non-specific inhibitor of phosphodiesterases, which leads to an increase in cAMP by preventing its degradation. The resultant rise in cAMP can activate THEG if it operates under cAMP-regulated mechanisms. | ||||||
Anisomycin | 22862-76-6 | sc-3524 sc-3524A | 5 mg 50 mg | $99.00 $259.00 | 36 | |
Anisomycin is a potent activator of stress-activated protein kinases, which can lead to the activation of THEG if it is a substrate or is regulated by these kinases during stress response. | ||||||
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 is a potent activator of protein kinase C (PKC). PKC activation can lead to phosphorylation and subsequent activation of THEG if THEG is a substrate or is regulated by PKC signaling pathways. | ||||||
BAY 60-6583 | 910487-58-0 | sc-503262 | 10 mg | $210.00 | ||
BAY 60-6583 selectively activates adenosine A2B receptors, which can increase intracellular cAMP levels via Gs protein signaling, possibly leading to activation of THEG if it is regulated by cAMP or PKA pathways. | ||||||
Zaprinast (M&B 22948) | 37762-06-4 | sc-201206 sc-201206A | 25 mg 100 mg | $105.00 $250.00 | 8 | |
Zaprinast inhibits phosphodiesterase 5, resulting in increased cAMP and cGMP levels. Elevated cGMP can lead to cross-activation of cAMP pathways, which may activate THEG if it is influenced by these cyclic nucleotides. | ||||||
Rolipram | 61413-54-5 | sc-3563 sc-3563A | 5 mg 50 mg | $77.00 $216.00 | 18 | |
Rolipram selectively inhibits phosphodiesterase 4, causing an increase in cAMP levels. This boost in cAMP may activate THEG if it is part of or regulated by cAMP-dependent pathways. | ||||||
Vardenafil | 224785-90-4 | sc-362054 sc-362054A sc-362054B | 100 mg 1 g 50 g | $526.00 $735.00 $16653.00 | 7 | |
Vardenafil, a phosphodiesterase 5 inhibitor, increases cGMP levels which can have an indirect effect on cAMP signaling. This may lead to activation of THEG if cAMP or PKA signaling modulates its activity. | ||||||
Cilostazol | 73963-72-1 | sc-201182 sc-201182A | 10 mg 50 mg | $109.00 $322.00 | 3 | |
Cilostazol inhibits phosphodiesterase 3, leading to increased cAMP in cells. This increase in cAMP could lead to activation of THEG if THEG is cAMP-responsive or regulated by downstream targets of cAMP such as PKA. | ||||||