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Technical Data
| Formula | C16H15ClN4O2 |
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| Molecular Weight | 330.77 | CAS No. | 263707-16-0 | |
| Solubility (25°C)* | In vitro | DMSO | 66 mg/mL (199.53 mM) | |
| Ethanol | 17 mg/mL (51.39 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | ESI-09 is a specific exchange protein directly activated by cAMP (EPAC) inhibitor with IC50 of 3.2 μM and 1.4 μM for EPAC1 and EPAC2, respectively, >100-fold selectivity over PKA. | ||||
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| Targets |
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| 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. [1] ESI-09 significantly reduces intracellular and total bacterial counts in human umbilical vein endothelial cells. [2] 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. [3] | ||||
| In vivo | ESI-09 (10 mg/kg/d, i.p.), via pharmacological inhibition of EPAC1, protects WT C57BL/6 mice from fatal SFG rickettsiosis. [2] |
Protocol (from reference)
| Animal Study:[2] |
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References
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Customer Product Validation
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, , Brain Behav Immun, 2016, 58:118-129.
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Data from [Data independently produced by , , Biomed Pharmacother, 2019, 109:1268-1275]
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Data from [Data independently produced by , , Acta Diabetol, 2017, 54(6):581-591]
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Data from [Data independently produced by , , Inflammation, 2018, 41(3):1093-1103]
Selleck's ESI-09 has been cited by 10 publications
| Inhibition of exchange proteins directly activated by cAMP as a strategy for broad-spectrum antiviral development [ J Biol Chem, 2023, 299(6):104749] | PubMed: 37100284 |
| Terbutaline attenuates LPS-induced injury of pulmonary microvascular endothelial cells by cAMP/Epac signaling [ Drug Dev Res, 2021, 10.1002/ddr.21901] | PubMed: 34846077 |
| Knockdown of GPSM1 Inhibits the Proliferation and Promotes the Apoptosis of B-Cell Acute Lymphoblastic Leukemia Cells by Suppressing the ADCY6-RAPGEF3-JNK Signaling Pathway [ Pathol Oncol Res, 2021, 27:643376] | PubMed: 34257610 |
| Exchange protein directly activated by cAMP (Epac) 1 plays an essential role in stress-induced exercise capacity by regulating PGC-1α and fatty acid metabolism in skeletal muscle. [ Pflugers Arch, 2020, 472(2):195-216] | PubMed: 31955265 |
| Curcumin pretreatment protects against hypoxia/reoxgenation injury via improvement of mitochondrial function, destabilization of HIF-1α and activation of Epac1-Akt pathway in rat bone marrow mesenchymal stem cells [Wang X, et al. Biomed Pharmacother, 2019, 109:1268-1275] | PubMed: 30551377 |
| Protective Effect of Quercetin in LPS-Induced Murine Acute Lung Injury Mediated by cAMP-Epac Pathway [Wang XF, et al. Inflammation, 2018, 41(3):1093-1103] | PubMed: 29569077 |
| Activation of Epac alleviates inflammation and vascular leakage in LPS-induced acute murine lung injury [Wang X, et al. Biomed Pharmacother, 2017, 96:1127-1136] | PubMed: 29174852 |
| The microRNA-7-mediated reduction in EPAC-1 contributes to vascular endothelial permeability and eNOS uncoupling in murine experimental retinopathy. [Garcia-Morales V, et al. Acta Diabetol, 2017, 54(6):581-591] | PubMed: 28353063 |
| Bile Acids Control Inflammation and Metabolic Disorder through Inhibition of NLRP3 Inflammasome [Guo C, et al. Immunity, 2016, 45(4):944] | PubMed: 27760343 |
| Cannabinoid receptor-2 stimulation suppresses neuroinflammation by regulating microglial M1/M2 polarization through the cAMP/PKA pathway in an experimental GMH rat model [Tao Y, et al. Brain Behav Immun, 2016, 10.1016/j.bbi.2016.05.020] | PubMed: 27261088 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.