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Merck
CN

SML1907

ESI-05

≥98% (HPLC)

Synonym(s):

1,3,5-Trimethyl-2-[(4-methylphenyl)sulfonyl]-benzene, Mesityl (4-methylphenyl) sulfone

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About This Item

Empirical Formula (Hill Notation):
C16H18O2S
CAS Number:
Molecular Weight:
274.38
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

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 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.


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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