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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
20 Results for "
EPAC1
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "EPAC1" in MCE Product Catalog:
10
10 Publications Verification
Cat. No.: HY-16704
CAS No.: 263707-16-0
Target:
Domaines de recherche:
ESI-09 is a novel noncyclic nucleotide EPAC antagonist with IC50 values of 3.2 and 1.4 μM for EPAC1 and EPAC2, respectively.
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2 Cited Publications
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CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.
1
1 Cited Publications
Synonyms: 8-CPT-2'-O-Me-cAMP sodium
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Domaines de recherche:
8-pCPT-2′-O-Me-cAMP (8-CPT-2'-O-Me-cAMP) sodium, an analog of cAMP, is an activator of exchange proteins activated by cAMP (Epac). 8-pCPT-2′-O-Me-cAMP sodium activates Epac1 (EC50 = 2.2 μM), but not PKA (EC50 >10 μM). 8-pCPT-2′-O-Me-cAMP sodium stimulates Epac-mediated Ca 2+ release in pancreatic β-cells in vitro. 8-pCPT-2′-O-Me-cAMP sodium is a Rap1 activator. 8-pCPT-2′-O-Me-cAMP sodium enhances the retinal pigment epithelium barrier against the pathological choroidal endothelial cell invasion that occurs in macular degeneration [1] .
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1 Cited Publications
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Domaines de recherche:
ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC50 of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation [1].
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1 Cited Publications
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HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP [1].
1
1 Cited Publications
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(R)-CE3F4 is a potent and selective inhibitor of exchange protein directly activated by cAMP isoform 1 (Epac1), with an IC50 of 4.2 μM, with 10-fold selectivity for Epac1 over Epac2 (IC50, 44 μM). (R)-CE3F4 is more potent than racemic CE3F4 and (S)-CE3F4 [1].
1
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AM-001 is a non-competitive inhibitor of Epac1 that blocks the activation of Rap1, a downstream effector of Epac1, in cultured cells. AM-001 can be used in heart disease-related research [1].
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I942 is a first in class, selective non-cyclic nucleotide (NCN) EPAC1 agonist. I942 can attenuate proinflammatory cytokine signalling normally associated with cardiovascular diseases [1].
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EPAC 5376753, a 2-Thiobarbituric acid (HY-77962) derivative, is a selective and allosteric Epac inhibitor. EPAC 5376753 inhibits Epac1 with an IC50 of 4 µM in Swiss 3T3 cells. EPAC 5376753 does not inhibit PKA and adenylyl cyclases [1].
Cat. No.: HY-134299
CAS No.: 663941-66-0
Synonyms: 8-(4-Chlorophenylthio)-cAMP-AM
Domaines de recherche:
8-CPT-cAMP-AM (8-(4-Chlorophenylthio)-cAMP-AM) is an Epac/PKA activator. 8-CPT-cAMP-AM potentiates glucose-dependent first- and second-phase insulin secretion, induces β-cell depolarization, modulates intracellular calcium via influx and ryanodine-sensitive store mobilization, and facilitates calcium-induced calcium release resistant to PKA inhibition. 8-CPT-cAMP-AM can be used for the research of cardiac hypertrophy, diabetic cardiomyopathy, and melanoma [1] .
Cat. No.: HY-116312
CAS No.: 510774-50-2
Synonyms: 8-CPT-2'-O-Me-cAMP
Target:
Domaines de recherche:
8-pCPT-2′-O-Me-cAMP (8-CPT-2'-O-Me-cAMP), an analog of cAMP, is an activator of exchange proteins activated by cAMP (Epac). 8-pCPT-2′-O-Me-cAMP activates Epac1 (EC50 = 2.2 μM), but not PKA (EC50 >10 μM). 8-pCPT-2′-O-Me-cAMP stimulates Epac-mediated Ca 2+ release in pancreatic β-cells in vitro. 8-pCPT-2′-O-Me-cAMP is a Rap1 activator. 8-pCPT-2′-O-Me-cAMP enhances the retinal pigment epithelium barrier against the pathological choroidal endothelial cell invasion that occurs in macular degeneration [1] .
Cat. No.: HY-117064
CAS No.: 1801911-86-3
NY-0173 is an antagonist of Exchange proteins directly activated by cAMP (EPAC), with IC50s of 3.5 μM (EPAC2)and 4.0 μM (EPAC1) respectively. NY-0173 can be used to elucidate the biological functions of EPAC .
Cat. No.: HY-134308
CAS No.: 221905-51-7
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8-NBD-cAMP sodium is a fluorescently labeled cyclic adenosine phosphate (cAMP) analogue. 8-NBD-cAMP sodium retains a similar biological activity to cAMP, regulating their activity by binding to specific proteins such as EPACs or PKA. 8-NBD-cAMP sodium can be used in fluorescent competitive binding experiments to evaluate the binding affinity of newly synthesized EPAC1 agonists to EPAC1 proteins [1].
Cat. No.: HY-182273
CAS No.: 3106606-59-8
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DM243 is an EPAC1 activator and STAT3 modulator with an pIC50 of 4.769 for EPAC1. DM243 increases GTP-bound Rap1 levels in EPAC1-expressing cells. DM243 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM243 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing α-smooth muscle actin and Collagen I levels in lung fibroblasts. DM243 exhibits minimal cytotoxicity in normal human lung fibroblasts [1].
Cat. No.: HY-123795
CAS No.: 1801911-70-5
NY0123 is a EPAC1 inhibitor. NY0123 significantly inhibits the expression of EPAC1, phosphorylated AKT, phosphorylated ERK1/2 and phosphorylated VEGFR2. NY0123 inhibits angiogenesis and tumor growth of triple-negative breast cancer. NY0123 is applicable to relevant research on triple-negative breast cancer [1].
Cat. No.: HY-182274
CAS No.: 3106606-60-1
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Domaines de recherche:
DM245 is an EPAC1 activator and STAT3 phosphorylation inhibitor with a target pIC50 of 4.801. DM245 activates EPAC1 to increase Rap1-GTP levels, with no activation of EPAC2 or PKA. DM245 reduces IL-6/IL-6Rα-evoked STAT3 phosphorylation in endothelial cells. DM245 suppresses TGF-β1-induced fibroblast-to-myofibroblast transition, reducing αSMA and Collagen I levels. DM245 exhibits minimal cytotoxicity in normal human lung fibroblasts, with negligible loss of intact nuclei after 72 h exposure [1].
Cat. No.: HY-108539R
CAS No.: 143703-25-7
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Domaines de recherche:
CE3F4 (Standard) is the analytical standard of CE3F4 (HY-108539). This product is intended for research and analytical applications. CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.
Cat. No.: HY-RS11662
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Domaines de recherche:
RAPGEF3 Human Pre-designed siRNA Set A contains three designed siRNAs for RAPGEF3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-107543R
CAS No.: 634207-53-7
Synonyms: 8-CPT-2'-O-Me-cAMP sodium (Standard)
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Domaines de recherche:
8-pCPT-2′-O-Me-cAMP sodium (Standard) is the analytical standard of 8-pCPT-2′-O-Me-cAMP (sodium) (HY-107543). This product is intended for research and analytical applications. 8-pCPT-2′-O-Me-cAMP (8-CPT-2'-O-Me-cAMP) sodium, an analog of cAMP, is an activator of exchange proteins activated by cAMP (Epac). 8-pCPT-2′-O-Me-cAMP sodium activates Epac1 (EC50 = 2.2 μM), but not PKA (EC50 >10 μM). 8-pCPT-2′-O-Me-cAMP sodium stimulates Epac-mediated Ca2+ release in pancreatic β-cells in vitro. 8-pCPT-2′-O-Me-cAMP sodium is a Rap1 activator. 8-pCPT-2′-O-Me-cAMP sodium enhances the retinal pigment epithelium barrier against the pathological choroidal endothelial cell invasion that occurs in macular degeneration [1] .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
