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- ESI-09 263707-16-0

- ESI-09 263707-16-0
ESI-09 263707-16-0
产品描述 描述 ESI-09 is a specific exchange protein directly activated by cAMP (EPAC) inhibitor with IC50 of 3.2 μM and 1.4 μM for EPAC1 and EPAC2, respectively, >100-fold selectivity over PKA.
纯度 >98%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 别名 ESI 09外观 faint yellow to dark orange powder可溶性/溶解性 DMSO : 33.1 mg/mL (100 mM)
Ethanol : 6.6 mg/mL (20 mM)生物活性 靶点 EPAC2 ,EPAC1In vitro(体外研究) ESI-09, a novel non-cyclic nucleotide EPAC antagonist, that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic β cells. On the other hand, ESI-09 fails to suppress epidermal growth factor (EGF)-induced phosphorylation of Akt in AsPC1 cells. In pancreatic cancer cells, ESI-09 inhibits cells migration and invasion through decreasing 007-AM-induced cell adhesion dose-dependently. ESI-09 significantly reduces intracellular and total bacterial counts in human umbilical vein endothelial cells. ESI-09 effectively antagonizes Schwann cells (SC) differentiation induced by CPT-cAMP as well as the formation of myelin. In SC-neuron cultures, ESI-09 dramatically reduces the number of O1 positive and MBP positive SCs without compromising the health of the neurons or the SCs themselves.In vivo(体内研究) ESI-09 (10 mg/kg/d, i.p.), via pharmacological inhibition of EPAC1, protects WT C57BL/6 mice from fatal SFG rickettsiosis.参考文献 参考文献 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.
研究领域 研究领域 Signal TransductionSecond MessengerNucleotide MessengercAMPSignal TransductionSecond MessengerNucleotide MessengercGMPDrug DiscoverySmall Molecule DrugLead Compound DiscoveryESI-09 263707-16-0温馨提示:本产品仅作科研实验使用,不支持临床等研究
