| Description | 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. |
| In vitro | 在WT C57BL/6小鼠中,ESI-09（10 mg/kg/d, i.p. ）通过对EPAC1的抑制作用,避免SFG立克次氏体病. |
| In vivo | ESI-09能够特异性抑制细胞内EPAC介导的Rap1活化和Akt磷酸化,以及EPAC介导的胰腺β细胞中胰岛分泌。在007-AM诱导的胰腺癌细胞中,ESI-09降低细胞的粘附性,同时抑制细胞的迁移。在CPT-cAMP诱导的Schwann细胞中,ESI-09能够显著抑制细胞分化和髓鞘的形成。在SC神经元培养基中, ESI-09显著降低O1阳性和MBP阳性的数量。 |
| Target activity | EPAC1:3.2 μM, EPAC2:1.4 μM |
| molecular weight | 330.77 |
| Molecular formula | C16H15ClN4O2 |
| CAS | 263707-16-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 33.1 mg/mL (100 mM) Ethanol: 6.6 mg/mL (20 mM) |
| References | 1. Almahariq M , et al. Mol Pharmacol. 2013, 83(1), 122-128. 2. Gong B, et al. Proc Natl Acad Sci U S A. 2013, 110(48), 19615-19620. 3. Bacallao K, et al. PLoS One. 2013, 8(12), e82354. 4. Xu C, Zhao W, Huang X, et al. TORC2/3-mediated DUSP1 upregulation is essential for human decidualization[J]. Reproduction. 2021, 1(aop). |
| Citations | 1. Xu C, Zhao W, Huang X, et al. TORC2/3-mediated DUSP1 upregulation is essential for human decidualization. Reproduction. 2021, 1(aop). 2. Zhao W, Xu C, Peng L, et al.cAMP/PKA signaling promotes AKT deactivation by reducing CIP2A expression, thereby facilitating decidualization.Molecular and Cellular Endocrinology.2023: 111946. 3. Cui S, Suo N, Yang Y, et al.The aminosteroid U73122 promotes oligodendrocytes generation and myelin formation.Acta Pharmacologica Sinica.2023: 1-12. |