ESI-09
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
ESI-09是EPAC的特异性抑制剂,对EPAC2和EPAC1的IC50值分别为1.4和3.2 M[1].
cAMP/cAMP调控的鸟苷酸交换因子(EPAC/cAMP-GEF)是一种响应于胞内cAMP的小GTPases Rap1和Rap2的鸟苷酸交换因子[2].
ESI-09是一种EPAC的特异性抑制剂.ESI-09(25 M)在25 M的cAMP存在时可将EPAC1和EPAC2 GEF活性降低到基础水平.在25 M的cAMP存在时,ESI-09可抑制cAMP介导的EPAC2和EPAC1 GEF活性,IC50值分别为1.4和3.2 M,比对PKA的选择性强100倍.在胰腺癌细胞系AsPC-1中,ESI-09可剂量依赖地抑制007-AM刺激的Akt T308和S473的磷酸化.在胰腺内分泌β细胞中,ESI-09可以剂量依赖的方式抑制007-AM刺激的胰岛素分泌增加.在胰腺癌细胞系AsPC-1和PANC-1中,ESI-09可通过抑制EPAC1显著减少细胞迁移[1].在20 M的cAMP存在时,ESI-09可抑制cAMP介导的EPAC2和EPAC1 GEF活性,IC50值分别为4.4和10.8 M[2].
参考文献:
[1]. Almahariq M, Tsalkova T, Mei FC, et al. A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion. Mol Pharmacol, 2013, 83(1): 122-128.
[2]. Zhu Y, Chen H, Boulton S, et al. Biochemical and pharmacological characterizations of ESI-09 based EPAC inhibitors: defining the ESI-09 ""therapeutic window"". Sci Rep, 2015, 5: 9344.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 330.77 |
Cas No. | 263707-16-0 |
Formula | C16H15ClN4O2 |
Solubility | ≥33.1 mg/mL in DMSO; insoluble in H2O; ≥2.22 mg/mL in EtOH with ultrasonic |
Chemical Name | (1E)-2-(5-tert-butyl-1,2-oxazol-3-yl)-N-(3-chloroanilino)-2-oxoethanimidoyl cyanide |
SDF | Download SDF |
Canonical SMILES | CC(C)(C)C1=CC(=NO1)C(=O)C(=NNC2=CC(=CC=C2)Cl)C#N |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1,2]: | |
细胞系 |
AsPC-1和PANC-1胰腺癌细胞,INS-1细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于16.6 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
10 μM,5分钟 |
应用 |
在AsPC-1胰腺癌细胞中,ESI-09(1 μM,10μM,5分钟)抑制EPAC介导的Akt磷酸化。在INS-1细胞中,ESI-09(5 μM,10 μM)抑制EPAC2介导的胰岛素分泌。ESI-09(5 μM,10 μM)抑制胰腺癌迁移。在AcPC-1和PANC-1细胞中,ESI-09预处理15分钟以剂量依赖性方式降低了007-AM诱导的细胞粘附。ESI-09显著降低人脐静脉内皮细胞的细胞内和细菌总数。 |
动物实验 [2]: | |
动物模型 |
C57BL/6 Epac1缺失小鼠 |
给药剂量 |
腹腔注射,10 mg/kg/d,5天 |
应用 |
ESI-09 (10 mg/kg/d, i.p.)治疗5天通过药理学抑制EPAC1,保护野生型C57BL/6小鼠免死于致命的SFG立克次体症。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Almahariq M, Tsalkova T, Mei F C, et al. A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion[J]. Molecular pharmacology, 2013, 83(1): 122-128. [2]. Gong B, Shelite T, Mei F C, et al. Exchange protein directly activated by cAMP plays a critical role in bacterial invasion during fatal rickettsioses[J]. Proceedings of the National Academy of Sciences, 2013, 110(48): 19615-19620. |
质量控制和MSDS
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