epac

Torbafylline, a xanthine derivative, is a phosphodiesterase (PDE) inhibitor that attenuates burn-induced protein hydrolysis in rat skeletal muscle through activation of the PDE4 cAMP EPAC PI3K Akt pathway, and inhibits the enhanced ubiquitin-proteasome-dependent protein hydrolysis in skeletal muscle of cancer- and sepsis-prone rats.

EPAC 5376753 is an allosteric inhibitor of EPAC1 with an IC50 of 4 µM in Swiss 3T3 cells.

Epacadostat (INCB 024360) is an oral, potent and selective IDO1 inhibitor with IC50 value of 71.8 nM.

Mepacrine (Erion) is an acridine derivative formerly widely used as an antimalarial. It is used in cell biological experiments as an inhibitor of phospholipase A2.

Isoxepac (Olopatadine USP Related Compound C) is a non-steroidal anti-antiphlogistic agent and analgesic.

Millepachine is a natural product found in the Chinese herbal medicine with strong antitumor effects against numerous human cancer cells.

Epacmarstobart (FSI-189; GS-0189) is a chimeric humanized IgG1κ antibody targeting mouse Signal Regulatory Protein Alpha (SIRPA).

ESI-09 is a new-typel noncyclic nucleotide EPAC antagonist.The IC50 values of ESI-09 for EPAC1 and EPAC2 is 3.2 and 1.4 μM, respectively.

ESI-08 is an effective antagonist of EPAC2 with an IC50 of 8.4 μM. ESI-08 selectively blocks cAMP-induced EPAC activation but not cAMP-mediated PKA activation.

HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 is an effective exchange protein. Which straightly activated by cAMP (Epac) antagonist (IC50=5.9 μM for Epac2).

8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA) and a potent inhibitor of cyclic GMP-specific phosphodiesterase (PDE VA) with an inhibitory concentration (IC50) of 0.9 μM. It also inhibits PDE III and PDE IV while significantly activating Epac, demonstrating diverse pharmacological activities [1] [2].

8-CPT-2Me-cAMP sodium is a sodium salt compound that selectively activates exchange proteins activated by cAMP (Epac), which are cAMP-sensitive guanine nucleotide exchange factors (GEFs) responsible for activating small GTPases Rap1 and Rap2. It specifically activates Epac1 with an EC50 value of 2.2 μM, while showing no activation of PKA with an EC50 value greater than 10 μM [1]. Additionally, 8-CPT-2Me-cAMP sodium stimulates the Epac-mediated release of calcium ions (Ca2+) in vitro in pancreatic β-cells [2].

Epac activator

NY0123 is an active EPAC antagonist with low micromolar inhibitory activity.

2'-O-Me-cAMP is an analog of the natural signaling molecule cAMP and serves as a selective activator for the cAMP-activated exchange factor (Epac), characterized by its low membrane permeability.

8-pMeOPT-2'-O-Me-cAMP is an analog of the signaling molecule cAMP and serves as an effective stimulator of the cAMP-activated exchange factors (Epac). Unlike cAMP, it does not activate PKA.

Sp-6-Phe-cAMPS is an effective activator of cAMP-dependent protein kinase (PKA) with site selectivity and membrane permeability. It does not activate the exchange factors directly stimulated by cAMP, making it suitable as a negative control for Epac. Sp-6-Phe-cAMPS can also be utilized in research on neurodegenerative diseases.

8-pCPT-5'-AMP is a lipophilic activator for PKA, PKG, and Epac (cAMP-activated exchange proteins), and serves as an analog of 5'-AMP.

8-Br-2'-O-Me-cAMP is an analog of the signaling molecule cAMP. It acts as an agonist for cAMP-activated exchange factors (Epac), yet unlike cAMP, it does not activate PKA.

6-Bn-cAMP is a selective activator of cAMP-dependent protein kinase (PKA) that does not activate Epac. Compared to cAMP, 6-Bn-cAMP enhances hydrolytic stability against PDE, esterases, and amidases, and significantly increases membrane permeability.

8-CPT-cAMP-AM is a highly membrane-permeable analog of the signaling molecule cAMP. It serves as an activator for both cAMP and cGMP-dependent protein kinases, as well as Epac (exchange protein activated by cAMP).

8-Br-cAMP-AM, an analog of cyclic adenosine monophosphate (cAMP), activates two principal signaling pathways in the heart by mimicking the action of cAMP: protein kinase A (PKA) and the guanine nucleotide exchange factor (Epac) directly activated by cAMP. This compound is employed in the study of cardiac ischemia and reperfusion injury.

8-pHPT-2'-O-Me-cAMP is an analog of cAMP and acts as an Epac agonist. This compound is utilized in cardiac-related research.

Sp-8-Br-2'-O-Me-cAMPS is a cAMP analog and an EPAC activator commonly used in metabolic-related research.