All Photos(1)
1,3,5-Trimethyl-2-[(4-methylphenyl)sulfonyl]-benzene, Mesityl (4-methylphenyl) sulfone
C16H18O2S
Recommended Products
Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
room temp
SMILES string
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
Application
ESI-05 has been used to study the effect of protein exchange directly activated by cAMP 2 on traumatic brain injury.
Biochem/physiol Actions
ESI-05 is a selective inhibitor against cAMP-regulated guanine nucleotide exhange factor (GEF) EPAC2 (Exchange factor directly activated by cAMP 2) activation by targeting an EPAC2-specific allosteric site at the interface of the two cAMP-binding domains. ESI-05 inhibits EAPC2, but not EPAC1 or PKA, activation by cAMP in a highly potent (IC50 = 430 nM; 25 μM cAMP) and cAMP-competitive manner in cell-free assays, and suppresses cAMP analog 007-AM-induced cellular Rap1 activation in EPAC2-, but not EPAC1-, expressing HEK293 transfectants.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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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.
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
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
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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