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Submit ReviewESI 09 is an EPAC inhibitor. Inhibits EPAC-mediated insulin release from pancreatic β cells. Selective for EPAC over PKA. ESI 09 decreases migration and invasion of AsPc-1 and PANC-1 pancreatic cancer cells in vitro.
ESI 09 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 330.77 |
公式 | C16H15ClN4O2 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 263707-16-0 |
PubChem ID | 6077765 |
InChI Key | DXEATJQGQHDURZ-DEDYPNTBSA-N |
Smiles | CC(C)(C)C1=CC(C(/C(C#N)=N/NC2=CC=CC(Cl)=C2)=O)=NO1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 33.08 | 100 | |
ethanol | 6.62 | 20 |
以下数据基于产品分子量 330.77。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.02 mL | 15.12 mL | 30.23 mL |
5 mM | 0.6 mL | 3.02 mL | 6.05 mL |
10 mM | 0.3 mL | 1.51 mL | 3.02 mL |
50 mM | 0.06 mL | 0.3 mL | 0.6 mL |
参考文献是支持产品生物活性的出版物。
Almahariq et al (2013) A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion. Mol.Pharmacol. 83 122 PMID: 23066090
If you know of a relevant reference for ESI 09, please let us know.
关键词: ESI 09, ESI 09 supplier, ESI09, EPAC, exchange, proteins, inhibitors, inhibits, GTPases, Rap, guanine, nucleotide, factor, cAMP, GEFI, 4773, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 ESI 09 的部分引用包括:
Derek C et al (2021) Regulation of Mitochondrial Function by Epac2 Contributes to Acute Inflammatory Hyperalgesia. J Neurosci 41 2883-2898 PMID: 33593853
Ginam et al (2021) β2-adrenergic receptor regulates ER-mitochondria contacts. Sci Rep 11 21477 PMID: 34728663
Cheng-Mao et al (2018) The EPAC-Rap1 pathway prevents and reverses cytokine-induced retinal vascular permeability. J Biol Chem 293 717-730 PMID: 29158262
Jeremy F et al (2019) Omega-3 Fatty Acids Activate Ciliary FFAR4 to Control Adipogenesis. Cell 179 1289-1305.e21 PMID: 31761534
Siddharth et al (2019) Elevated glucose concentration in culture media decreases membrane trafficking of SGLT2 in LLC-PK1 cells via a cAMP/PKA-dependent pathway. Am J Physiol Cell Physiol 316 C913-C924 PMID: 30943059
Diana J et al (2019) Phospho-substrate profiling of Epac-dependent protein kinase C activity. Mol Cell Biochem 456 167-178 PMID: 30739223
Caglar et al (2019) Adenosine Receptor Signaling Targets Both PKA and Epac Pathways to Polarize Dendritic Cells to a Suppressive Phenotype. J Immunol 203 3247-3255 PMID: 31722989
Chris et al (2020) Neuronal hyperexcitability is a DLK-dependent trigger of herpes simplex virus reactivation that can be induced by IL-1. Elife 9 PMID: 33350386
Alyson E et al (2020) Polypharmacological Perturbation of the 14-3-3 Adaptor Protein Interactome Stimulates Neurite Outgrowth. Cell Chem Biol 27 657-667.e6 PMID: 32220335
Perkins et al (2018) Autocrine-paracrine prostaglandin E2 signaling restricts TLR4 internalization and TRIF signaling. Nat.Immunol. 19 1309 PMID: 30397349
Guichard et al (2017) Anthrax edema toxin disrupts distinct steps in Rab11-dependent junctional transport. PLoS Pathog 13 e1006603 PMID: 28945820
Drelich et al (2018) Exchange Protein Directly Activated by cAMP Modulates Ebola Virus Uptake into Vascular Endothelial Cells. Viruses 10 PMID: 30332733
Wang et al (2015) A pivotal role of FOS-mediated BECN1/Beclin 1 upregulation in DA D2 and D3 receptor agonist-induced autophagy activation. EMBO Mol Med 11 2057 PMID: 26649942
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