[CAS NO. 263707-16-0]  ESI-09

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PRODUCTS SPECIFICATIONS [263707-16-0]

Catalog
SLK-S7499
Brand
Selleck
CAS
263707-16-0

DESCRIPTION [263707-16-0]

Overview

MDL-
Molecular Weight330.77
Molecular FormulaC16H15ClN4O2
SMILESO=C(C1=NOC(C(C)(C)C)=C1)/C(C#N)=N/NC2=CC(Cl)=CC=C2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM3.0232 mL15.1162 mL30.2325 mL
5 mM0.6046 mL3.0232 mL6.0465 mL
10 mM0.3023 mL1.5116 mL3.0232 mL
50 mM0.0605 mL0.3023 mL0.6046 mL

Description

ESI-09 is a specific inhibitor with of 3.2 μM and 1.4 μM for EPAC1 and EPAC2, respectively, >100-fold selectivity over PKA.

Targets

EPAC2 [1]
(Cell-free assay)
EPAC1 [1]
(Cell-free assay)
1.4 μM3.2 μM

In vitro

ESI-09, a novel non-cyclic nucleotide EPAC antagonist, that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic β cells. On the other hand, ESI-09 fails to suppress epidermal growth factor (EGF)-induced phosphorylation of Akt in AsPC1 cells. In pancreatic cancer cells, ESI-09 inhibits cells migration and invasion through decreasing 007-AM-induced cell adhesion dose-dependently. ESI-09 significantly reduces intracellular and total bacterial counts in human umbilical vein endothelial cells. ESI-09 effectively antagonizes Schwann cells (SC) differentiation induced by CPT-cAMP as well as the formation of myelin. In SC-neuron cultures, ESI-09 dramatically reduces the number of O1 positive and MBP positive SCs without compromising the health of the neurons or the SCs themselves.

In vivo

ESI-09 (10 mg/kg/d, i.p.), via pharmacological inhibition of EPAC1, protects WT C57BL/6 mice from fatal SFG rickettsiosis.