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ESI-09

CAS No. : 263707-16-0

MCE 站：ESI-09

产品活性：ESI-09是新型非环状核苷酸EPAC的拮抗剂，抑制EPAC1 ａnd EPAC2的IC₅₀值分别为3.2和1.4 μM。

研究领域：Anti-infection

作用靶点：Virus Protease

In Vitro: While cAMP competes with 8-NBD-cAMP binding with an IC₅₀ of 39 µM, ESI-09 shows an increased potency with an apparent IC₅₀ of 10 µM. ESI-09 inhibis cAMP-mediated EPAC2 ａnd EPAC1 GEF activity with an IC₅₀ of 1.4 ａnd 3.2µM, respectively. ESI-09 could fit well into the functional cAMP-binding pocket of EPAC1, establishing favorable hydrophobic ａnd hydrogen bonding interactions with the protein’s active-site residues. ESI-09 inhibits 007-AM-stimulated Akt phosphorylation at T308 ａnd S473 in a dose-dependent manner. ESI-09 inhibits pancreatic cancer cells AsPC-1 ａnd PANC-1 migration. ESI-09 inhibits EPAC1-mediated adhesion of PDA cells on collagen I. Exposure to ESI-09 significantly reduces intracellular ａnd total bacterial counts in HUVECs at 30 min postinfection with 10 multiplicities of infection (MOI) of R. australis compared with similarly infected controls.

In Vivo: Treatment with ESI-09 dramatically protects WT mice against R. australis infection with much milder disease manifestations ａnd significantly improves survival.

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