质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 20 mg/mL, clear
储存温度
room temp
SMILES字符串
CC1=CC=C(S(C2=C(C)C=C(C)C=C2C)(=O)=O)C=C1
InChI
1S/C16H18O2S/c1-11-5-7-15(8-6-11)19(17,18)16-13(3)9-12(2)10-14(16)4/h5-10H,1-4H3
InChI key
CGPHOZWFSFNOEQ-UHFFFAOYSA-N
应用
ESI-05已被用于研究cAMP 2直接激活的蛋白交换对颅脑损伤的作用。
生化/生理作用
ESI-05是一种靶向cAMP调节的鸟嘌呤核苷酸交换因子（GEF）EPAC2（直接由cAMP 2激活的交换因子）激活的选择性抑制剂，其可靶向两个cAMP结合域的交界面上的EPAC2特异性变构位点。在无细胞测定中，ESI-05可以高效地以与cAMP竞争的方式抑制cAMP对EAPC2的激活（IC50 = 430 nM；25 μM cAMP），但不可抑制EPAC1或PKA。同时，其可抑制表达EPAC2（而非EPAC1）的HEK293转染子中，cPAC类似物007-AM诱导的细胞Rap1的激活。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Eva Calderón-Sánchez et al.
PloS one, 11(2), e0147375-e0147375 (2016-02-04)
Urocortin-1 (Ucn-1) is an endogenous peptide that protects heart from ischemia and reperfusion (I/R) injuries. Ucn-1 is known to prevent cardiac cell death, but its role in the transcription of specific genes related to survival signaling pathway has not been
Tamara Tsalkova et al.
Proceedings of the National Academy of Sciences of the United States of America, 109(45), 18613-18618 (2012-10-24)
The major physiological effects of cAMP in mammalian cells are transduced by two ubiquitously expressed intracellular cAMP receptors, protein kinase A (PKA) and exchange protein directly activated by cAMP (EPAC), as well as cyclic nucleotide-gated ion channels in certain tissues.
Haijun Chen et al.
Journal of medicinal chemistry, 56(3), 952-962 (2013-01-05)
EPAC1 and EPAC2, two isoforms of exchange proteins directly activated by cAMP (EPAC), respond to the second messenger cAMP and regulate a wide variety of intracellular processes under physiological and pathophysiological circumstances. Herein, we report the chemical design, synthesis, and
Ling Zhang et al.
Frontiers in neuroscience, 12, 263-263 (2018-05-10)
Traumatic brain injury (TBI) is a major cause of mortality and disability worldwide. TBI-induced neuronal apoptosis is one of the main contributors to the secondary injury process. The aim of this study is to investigate the involvement of Exchange protein
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