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质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
, faint yellow to dark orange
溶解性
DMSO: 20 mg/mL, clear
储存温度
2-8°C
InChI
1S/C16H15ClN4O2/c1-16(2,3)14-8-12(21-23-14)15(22)13(9-18)20-19-11-6-4-5-10(17)7-11/h4-8,19H,1-3H3/b20-13+
InChI key
DXEATJQGQHDURZ-DEDYPNTBSA-N
应用
ESI-09 已被用作 cAMP 直接激活交换因子 (EPAC) 的拮抗剂。
生化/生理作用
ESI-09 是 EPAC（cAMP 直接激活的交换蛋白）的强效、特异性抑制剂。ESI-09 抑制 EPAC1 和 EPAC2，IC 50 值分别为 3.2 和 1.4μM，在 25μM 时对 PKA 无活性。在胰腺细胞系中，该化合物阻断 Akt 的磷酸化和胰岛素分泌。ESI-09 抑制胰腺癌细胞系的迁移。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
AKAP-mediated feedback control of cAMP gradients in developing hippocampal neurons.
Gorshkov K, et al.
Nature Chemical Biology, 13(4), 425-425 (2017)
Different cAMP sources are critically involved in G protein?coupled receptor CRHR1 signaling.
Inda C, et al.
The Journal of Cell Biology, 214(2), 181-195 (2016)
Transforming growth factor β2 promotes transcription of COX2 and EP4, leading to a prostaglandin E2-driven autostimulatory loop that enhances virulence of Theileria annulata transformed macrophages.
Haidar M, et al.
Infection and Immunity, 83(5), 1869-1880 (2015)
α-Viniferin Improves Facial Hyperpigmentation via Accelerating Feedback Termination of cAMP/PKA-Signaled Phosphorylation Circuit in Facultative Melanogenesis.
Yun C Y, et al.
Theranostics, 8(7), 2031-2031 (2018)
Wei Liu et al.
The Journal of experimental medicine, 217(4) (2020-01-10)
Progressive loss of retinal ganglion cells (RGCs) leads to irreversible visual deficits in glaucoma. Here, we found that the level of cyclic AMP and the activity and expression of its mediator Epac1 were increased in retinas of two mouse models
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