α-[2-(3-Chlorophenyl)hydrazinylidene]-5-(1,1-dimethylethyl)-b-oxo-3-isoxazolepropanenitrile
ESI-09
CAS: 263707-16-0
Molecular Formula: C16H15ClN4O2
α-[2-(3-Chlorophenyl)hydrazinylidene]-5-(1,1-dimethylethyl)-b-oxo-3-isoxazolepropanenitrile - Names and Identifiers
α-[2-(3-Chlorophenyl)hydrazinylidene]-5-(1,1-dimethylethyl)-b-oxo-3-isoxazolepropanenitrile - Physico-chemical Properties
| Molecular Formula | C16H15ClN4O2 |
| Molar Mass | 330.77 |
| Melting Point | >175°C (dec.) |
| Solubility | DMSO: ≥ 47 mg/mL |
| Appearance | powder |
| Color | , faint yellow to dark orange |
| Storage Condition | 2-8°C |
| In vitro study | ESI-09, a novel non-cyclic nucleotide EPAC antagonist capable of specifically blocking EPAC-mediated Rap1 activation and Akt phosphorylation in cells, as well as EPAC-mediated islet secretion in pancreatic beta cells. On the other hand, ESI-09 did not inhibit epidermal growth factor (EGF)-induced Akt phosphorylation in AsPC1 cells. In pancreatic cancer cells, ESI-09 inhibited cell migration and invasion by dose-dependently reducing 007-AM-induced cell adhesion. ESI-09 significantly reduced the total number of bacteria in human umbilical vein endothelial cells. ESI-09 effectively antagonized CPT-cAMP induced Schwann cell (SC) differentiation and myelination. In SC neuron medium, ESI-09 significantly reduced the number of o1-positive and MBP-positive without affecting the health of the neurons or SCs themselves. ESI-09, a novel acyclic nucleotide EPAC antagonist that specifically blocks EPAC-mediated Rap1 activation and Akt phosphorylation in cells, and EPAC-mediated islet secretion in pancreatic beta cells. On the other hand, ESI-09 did not inhibit epidermal growth factor (EGF)-induced Akt phosphorylation in AsPC1 cells. In pancreatic cancer cells, ESI-09 inhibited cell migration and invasion by dose-dependently reducing 007-AM-induced cell adhesion. ESI-09 significantly reduced the total number of bacteria in human umbilical vein endothelial cells. ESI-09 effectively antagonized CPT-cAMP induced Schwann cell (SC) differentiation and myelination. In SC neuron medium, ESI-09 significantly reduced the number of o1-positive and MBP-positive without affecting the health of the neurons or SCs themselves. |
| In vivo study | ESI-09 (10 mg/kg/d, I. p.) protects WT C57BL/6 mice from lethal SFG rickettsiosis by pharmacological inhibition of epac1. ESI-09 (10 mg/kg/d, I. p.) protects WT C57BL/6 mice from lethal SFG rickettsiosis by pharmacological inhibition of epac1. |
α-[2-(3-Chlorophenyl)hydrazinylidene]-5-(1,1-dimethylethyl)-b-oxo-3-isoxazolepropanenitrile - Risk and Safety
| WGK Germany | 3 |
α-[2-(3-Chlorophenyl)hydrazinylidene]-5-(1,1-dimethylethyl)-b-oxo-3-isoxazolepropanenitrile - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.023 ml | 15.116 ml | 30.233 ml |
| 5 mM | 0.605 ml | 3.023 ml | 6.047 ml |
| 10 mM | 0.302 ml | 1.512 ml | 3.023 ml |
| 5 mM | 0.06 ml | 0.302 ml | 0.605 ml |
Last Update：2024-01-02 23:10:35
α-[2-(3-Chlorophenyl)hydrazinylidene]-5-(1,1-dimethylethyl)-b-oxo-3-isoxazolepropanenitrile - Reference Information
| biological activity | ESI-09 is a specific exchange protein directly activated by cAMP (EPAC) inhibitor, its IC50 for EPAC1 and EPAC2 is 3.2 μM and 1.4 μM respectively, which is more than 100 times higher than PKA. ESI-09 is a specific exchange protein directly activated by cAMP (EPAC) inhibitor. Its IC50 for EPAC1 and EPAC2 is 3.2 μM and 1.4 μM, respectively, which is more than 100 times higher than PKA selectivity. |
| in vitro study | ESI-09, a new non-cyclic nucleotide EPAC antagonist can specifically block intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, and EPAC-mediated islet secretion in pancreatic β cells. On the other hand, ESI-09 did not inhibit epidermal growth factor (EGF)-induced Akt phosphorylation in AsPC1 cells. In pancreatic cancer cells, ESI-09 inhibit cell migration and invasion by dose-dependent reduction of 007-AM-induced cell adhesion. ESI-09 significantly reduced the total number of bacteria in human umbilical vein endothelial cells. ESI-09 effectively antagonized CPT-cAMP-induced differentiation of Schwann cells (SC) and myelin formation. In SC neuron medium, ESI-09 significantly reduced the number of O1 positive and MBP positive without affecting the health of neurons or SCs themselves. ESI-09, a novel non-cyclic nucleotide EPAC antagonist, can specifically block intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, and EPAC-mediated islet secretion in pancreatic β cells. On the other hand, ESI-09 did not inhibit epidermal growth factor (EGF)-induced Akt phosphorylation in AsPC1 cells. In pancreatic cancer cells, ESI-09 inhibit cell migration and invasion by dose-dependent reduction of 007-AM-induced cell adhesion. ESI-09 significantly reduced the total number of bacteria in human umbilical vein endothelial cells. ESI-09 effectively antagonized CPT-cAMP-induced differentiation of Schwann cells (SC) and myelin formation. In SC neuron medium, ESI-09 significantly reduced the number of O1 positive and MBP positive without affecting the health of neurons or SCs themselves. |
| in vivo study | ESI-09 (10 mg/kg/d, I. p.), through pharmacological inhibition of EPAC1, WT C57BL/6 mice were protected from fatal SFG rickettsia. ESI-09 (10 mg/kg/d, I. p.) protects WT C57BL/6 mice from fatal SFG rickettsiosis through pharmacological inhibition of EPAC1. |
| target | TargetValue EPAC2 (Cell-free assay) 1.4 μM EPAC1 (Cell-free assay) 3.2 μM |
| Target | Value |
| EPAC2 (Cell-free assay) | 1.4 μM |
| EPAC1 (Cell-free assay) | 3.2 μM |
Last Update：2024-04-09 21:54:55
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Product Name: 2-(5-(tert-butyl)isoxazol-3-yl)-N-(3-chlorophenyl)-2-oxoacetohydrazonoyl cyanide Request for quotation
CAS: 263707-16-0
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CAS: 263707-16-0
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
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Product Name: ESI-09 Visit Supplier Webpage Request for quotation
CAS: 263707-16-0
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CAS: 263707-16-0
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