epac

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

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.

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.

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 (GS-0189/FSI-189) is a humanized monoclonal antibody targeting Signal Regulatory Protein Alpha (SIRP alpha). SIRP alpha is an inhibitory receptor primarily expressed on myeloid cells, such as macrophages and dendritic cells. It suppresses phagocytosis by interacting with CD47 on the surface of tumor cells. Epacmarstobart specifically binds to SIRP alpha, blocking its interaction with CD47 and relieving the inhibitory signals in macrophages, thereby significantly enhancing the recognition and engulfment of cancer cells. The antibody is being evaluated in clinical trials for the treatment of various hematologic and solid malignancies.

Cepacin A is an alkyne antibiotic with antibacterial properties, exhibiting a minimum inhibitory concentration (MIC) of 0.2 μg/mL against Staphylococcus. Additionally, Cepacin A displays a degree of toxicity in mice, with an LD50 of 30 mg/kg when administered intraperitoneally.

Cepacin B displays activity against both Gram-positive and Gram-negative bacteria.

Quinacrine dihydrochloride (Mepacrine dihydrochloride) is the dihydrochloride salt of the 9-aminoacridine derivative quinacrine with potential antineoplastic and antiparasitic activities.

Choline chloride (Biocoline) is a basic constituent of lecithin that is found in many plants and animal organs. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism.

MAY0132 is a and highly selective inhibitor of exchange protein directly activated by cAMP 2 (EPAC2) with a measured IC50 of 0.4 μM, demonstrating over 100-fold selectivity over the EPAC1 isoform and exhibiting broad-spectrum antiviral efficacy against respiratory viruses including RSV, HMPV, and AdV.

[D-Trp7,9,10]-Substance P acetate is an analogue of substance P which inhibits ion conductance through nicotinic acetylcholine receptors.

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).

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.

CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1; IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively).

ESI-05 (NSC-116966) is a specific EPAC2 (exchange protein directly activated by cAMP 2) antagonist (IC50: 0.4 μM). ESI-05 inhibits cAMP-mediated activation of EPAC2, as well as EAPC2, mediated Rap1 activation.

Quinacrine Dihydrochloride Dihydrate is an orally available antimalarial agent capable of crossing the blood-brain barrier. It exhibits anticancer activity by inhibiting WNT/TCF and topoisomerase, inducing autophagy and apoptosis, and activating p53. Quinacrine is an acridine dye derivative used for DNA and RNA staining in fixed cells (Ex/Em=436/525 nm).

I942 is a novel, selective ACyclic nucleotide (NCN) EPAC1 agonist that activates exchange proteins to regulate inflammatory gene expression in human umbilical blood tubes and inhibit pro-inflammatory cytokine signaling associated with cardiovascular disease.

Quinacrine methanesulfonate is a bioactive chemical.

HJC0350 is an effective and specific EPAC2 inhibitor (IC50: 0.3 μM), and no inhibition of Epac1.

Isepamicin sulfate (sch21420) Sulphate) , an aminoglycoside antibacterial with good activity against strains producing type I 6-acetyltransferase, inhibits bacterial protein synthesis by targeting the bacterial 30S ribosomal subunit.

(D-Arg1,D-Pro2,D-Trp7,9,L-Leu11)-Substance P (acetate), an antagonist of Substance P and Bombesin, modulates ocular inflammatory responses triggered by antidromic trigeminal nerve stimulation [1].