CREBL2 Activators
CREBL2 can initiate a cascade of intracellular events that lead to its phosphorylation and activation. Forskolin acts directly on adenylyl cyclase, an enzyme that converts ATP to cyclic AMP (cAMP), which in turn activates protein kinase A (PKA). PKA is known to phosphorylate CREBL2, thereby potentially modulating its activity. Similarly, Isoproterenol, a beta-adrenergic agonist, and Epinephrine, a naturally occurring catecholamine, bind to beta-adrenoceptors, which are linked to Gs proteins. This interaction stimulates the production of cAMP by adenylyl cyclase. The rise in cAMP levels leads to PKA activation, which may also target CREBL2. Dopamine and Glucagon, by engaging their respective Gs protein-coupled receptors, initiate a similar process of cAMP-mediated PKA activation, with subsequent phosphorylation of CREBL2. Terbutaline and Salbutamol, both beta2-adrenergic agonists, further exemplify this mechanism by activating beta2-adrenergic receptors and promoting PKA-mediated phosphorylation of CREBL2.
In addition to these direct activators, several compounds can increase intracellular cAMP by inhibiting its degradation. IBMX, a non-specific phosphodiesterase inhibitor, and Rolipram, a selective phosphodiesterase 4 inhibitor, prevent the breakdown of cAMP, indirectly leading to sustained PKA activation and CREBL2 phosphorylation. Prostaglandin E1 (PGE1) operates through its receptors, EP2 and EP4, to activate Gs proteins and the subsequent adenylyl cyclase-mediated pathway. Histamine, through the H2 receptor, also increases cAMP levels, thereby facilitating PKA's role in CREBL2 regulation. Anisomycin, although different in its primary action as a protein synthesis inhibitor, is capable of activating stress-activated protein kinases like JNK, which can phosphorylate members of the CREB family, including CREBL2, albeit through a pathway distinct from the cAMP-PKA axis.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $76.00 $150.00 $725.00 $1385.00 $2050.00 | 73 | |
Forskolin directly activates adenylyl cyclase, leading to an increase in cyclic AMP (cAMP) levels. Elevated cAMP activates protein kinase A (PKA), which can then phosphorylate and activate CREBL2 as part of the cAMP response element-binding (CREB) family of transcription factors. | ||||||
Isoproterenol Hydrochloride | 51-30-9 | sc-202188 sc-202188A | 100 mg 500 mg | $27.00 $37.00 | 5 | |
Isoproterenol, a beta-adrenergic agonist, binds to beta-adrenoceptors, which couples to Gs proteins, leading to the activation of adenylyl cyclase, increasing cAMP levels, and subsequently activating PKA. PKA can phosphorylate CREBL2, enhancing its transcriptional activity. | ||||||
IBMX | 28822-58-4 | sc-201188 sc-201188B sc-201188A | 200 mg 500 mg 1 g | $159.00 $315.00 $598.00 | 34 | |
IBMX is a non-specific inhibitor of phosphodiesterases which degrade cAMP and cGMP. By inhibiting these enzymes, IBMX increases intracellular levels of cAMP, indirectly leading to PKA activation which can phosphorylate CREBL2. | ||||||
Rolipram | 61413-54-5 | sc-3563 sc-3563A | 5 mg 50 mg | $75.00 $212.00 | 18 | |
Rolipram is a selective inhibitor of phosphodiesterase 4 (PDE4), an enzyme that breaks down cAMP. By inhibiting PDE4, rolipram increases intracellular cAMP levels, which leads to PKA activation and potential phosphorylation of CREBL2. | ||||||
(−)-Epinephrine | 51-43-4 | sc-205674 sc-205674A sc-205674B sc-205674C sc-205674D | 1 g 5 g 10 g 100 g 1 kg | $40.00 $102.00 $197.00 $1739.00 $16325.00 | ||
Epinephrine interacts with beta-adrenergic receptors, activating the Gs protein and adenylyl cyclase, which results in increased cAMP production and PKA activation. Activated PKA may then phosphorylate CREBL2. | ||||||
Dopamine | 51-61-6 | sc-507336 | 1 g | $290.00 | ||
Dopamine can bind to dopamine receptors that are coupled to Gs proteins, leading to increased cAMP production by adenylyl cyclase. The rise in cAMP activates PKA, which may phosphorylate CREBL2. | ||||||
PGE1 (Prostaglandin E1) | 745-65-3 | sc-201223 sc-201223A | 1 mg 10 mg | $30.00 $142.00 | 16 | |
PGE1 binds to EP2 and EP4 receptors, which are coupled to Gs proteins, leading to increased cAMP levels and PKA activation. PKA can then phosphorylate CREBL2, enhancing its activity. | ||||||
Histamine, free base | 51-45-6 | sc-204000 sc-204000A sc-204000B | 1 g 5 g 25 g | $92.00 $277.00 $969.00 | 7 | |
Histamine can stimulate H2 receptors, which are coupled to Gs proteins, leading to an increase in intracellular cAMP levels and activation of PKA. PKA has the potential to phosphorylate CREBL2. | ||||||
Terbutaline Hemisulfate | 23031-32-5 | sc-204911 sc-204911A | 1 g 5 g | $90.00 $371.00 | 2 | |
Terbutaline is a beta2-adrenergic agonist that activates Gs protein-coupled receptors, increasing cAMP levels, thus leading to PKA activation. PKA can phosphorylate CREBL2. | ||||||
Salbutamol | 18559-94-9 | sc-253527 sc-253527A | 25 mg 50 mg | $92.00 $138.00 | ||
Salbutamol, a beta2-adrenergic agonist, binds to beta2-adrenergic receptors, activating the Gs protein and increasing adenylyl cyclase activity. This results in higher cAMP and PKA activation, which can phosphorylate CREBL2. | ||||||