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| 品牌 | absin | CAS | 263707-16-0 |
|---|---|---|---|
| 分子式 | C16H15ClN4O2 | 纯度 | ＞98% |
| 分子量 | 330.77 | 货号 | abs47027962 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is a specific exchange protein | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
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 ,EPAC1 |
| In 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 |
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| 研究领域 | |
| 研究领域 | Signal TransductionSecond MessengerNucleotide MessengercAMP Signal TransductionSecond MessengerNucleotide MessengercGMP Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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