340817-81-4
Chemical Structure
AM-001
- CAS No.: 340817-81-4
- Formula:C24H16FN3OS2
- Molecular Weight:445.53
IUPAC Name: 3-amino-N-(4-fluorophenyl)-4-phenyl-6-(thiophen-2-yl)thieno[2,3-b]pyridine-2-carboxamide
InChIKey: KOJCITYQTOGCGM-UHFFFAOYSA-N
SMILES: NC1=C(C(NC2=CC=C(F)C=C2)=O)SC3=C1C(C4=CC=CC=C4)=CC(C5=CC=CS5)=N3
Biological Activity: AM-001 is a selective Epac1 inhibitor with an IC50 value of 47.8-53.7 μM. AM-001 blocks cAMP (Cyclic AMP) (HY-B1511)-induced conformational changes of Epac1, inhibits Epac1-dependent activation of Rap1, and does not compete with cAMP for binding to Epac1. AM-001 disrupts the formation of the Epac1-GRK5 complex, blocks nuclear import of GRK5, and inhibits GRK5-mediated nuclear export of HDAC5 and activation of MEF2. AM-001 can be used in research related to heart disease, myocardial ischemia/reperfusion injury, SARS-CoV-2 infection, influenza A virus infection, atrial fibrillation and idiopathic pulmonary fibrosis[1][2][3][4].
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AM-001 | 99.95% | AM-001 is a selective Epac1 inhibitor with an IC50 value of 47.8-53.7 μM. AM-001 blocks cAMP (Cyclic AMP) (HY-B1511)-induced conformational changes of Epac1, inhibits Epac1-dependent activation of Rap1, and does not compete with cAMP for binding to Epac1. AM-001 disrupts the formation of the Epac1-GRK5 complex, blocks nuclear import of GRK5, and inhibits GRK5-mediated nuclear export of HDAC5 and activation of MEF2. AM-001 can be used in research related to heart disease, myocardial ischemia/reperfusion injury, SARS-CoV-2 infection, influenza A virus infection, atrial fibrillation and idiopathic pulmonary fibrosis. | ||||||||||||||||||||
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References
- [1]. Laudette M, et al. Identification of a pharmacological inhibitor of Epac1 that protects the heart against acute and chronic models of cardiac stress. Cardiovascular research. 2019 Oct 01;115(12):1766-1777. [Content Brief]
- [2]. Foret-Lucas C, et al. EPAC1 Pharmacological Inhibition with AM-001 Prevents SARS-CoV-2 and Influenza A Virus Replication in Cells. Viruses. 2023 Jan 23;15(2):319.
- [3]. Boileve A, et al. Deciphering pro-arrhythmogenic mechanisms of EPAC in human atrial cardiomyocytes. The Journal of physiology. 2025 Oct 09. [Content Brief]
- [4]. Jankowski K, et al. Pharmacological inhibition of Epac1 protects against pulmonary fibrosis by blocking FoxO3a neddylation. The European respiratory journal. 2025 Oct;66(4):2402250.
