ESI 09 - ≥98%(HPLC), high purity , CAS No.263707-16-0, Inhibitor of Rap guanine nucleotide exchange factor 3;Inhibitor of Rap guanine nucleotide exchange factor 4

Item Number
E288332
Grouped product items
SKUSizeAvailabilityPrice Qty
E288332-5mg
5mg
In stock
$70.90
E288332-10mg
10mg
In stock
$113.90
E288332-50mg
50mg
In stock
$423.90
E288332-100mg
100mg
In stock
$641.90

Epac inhibitor

Basic Description

Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsEPAC inhibitor. Inhibits EPAC-mediated insulin releases from pancreaticβcells. Selective for EPAC over PKA. Decreases migration and invasion of AsPc-1 and PANC-1 pancreatic cancer cellsin vitro.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of Rap guanine nucleotide exchange factor 3;Inhibitor of Rap guanine nucleotide exchange factor 4
Product Description

product 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.

Associated Targets(Human)

RAPGEF3 Tchem Rap guanine nucleotide exchange factor 3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
RAPGEF4 Tchem Rap guanine nucleotide exchange factor 4 (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ALB Tchem Serum albumin (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ALB Tchem Serum albumin (2651 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK293 (82097 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRPM7 Tchem Transient receptor potential cation channel subfamily M member 7 (19 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RAPGEF3 Tchem Rap guanine nucleotide exchange factor 3 (15528 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RAPGEF4 Tchem Rap guanine nucleotide exchange factor 4 (11476 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HepG2-CD81 (19978 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Pseudomonas aeruginosa (123386 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Klebsiella pneumoniae (43867 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Staphylococcus aureus (210822 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Acinetobacter baumannii (41033 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Escherichia coli (133304 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Cryptococcus neoformans (21258 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Candida albicans (78123 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Plasmodium berghei (192651 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Names and Identifiers

IUPAC Name (1E)-2-(5-tert-butyl-1,2-oxazol-3-yl)-N-(3-chloroanilino)-2-oxoethanimidoyl cyanide
INCHI InChI=1S/C16H15ClN4O2/c1-16(2,3)14-8-12(21-23-14)15(22)13(9-18)20-19-11-6-4-5-10(17)7-11/h4-8,19H,1-3H3/b20-13+
InChi Key DXEATJQGQHDURZ-DEDYPNTBSA-N
Canonical SMILES CC(C)(C)C1=CC(=NO1)C(=O)C(=NNC2=CC(=CC=C2)Cl)C#N
Isomeric SMILES CC(C)(C)C1=CC(=NO1)C(=O)/C(=N/NC2=CC(=CC=C2)Cl)/C#N
PubChem CID 6077765
Molecular Weight 330.77

Certificates

Certificate of Analysis(COA)

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4 results found

Lot NumberCertificate TypeDateItem
J2130395Certificate of AnalysisAug 14, 2024 E288332
J2130396Certificate of AnalysisAug 14, 2024 E288332
J2130397Certificate of AnalysisAug 14, 2024 E288332
J2130511Certificate of AnalysisAug 14, 2024 E288332

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 33.08, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 6.62, Max Conc. mM: 20

Related Documents

References

1. Almahariq M, Tsalkova T, Mei FC, Chen H, Zhou J, Sastry SK, Schwede F, Cheng X.  (2013)  A novel EPAC-specific inhibitor suppresses pancreatic cancer cell migration and invasion..  Mol Pharmacol,  83  (1): (122-8).  [PMID:23066090]
2. Tsalkova T, Mei FC, Li S, Chepurny OG, Leech CA, Liu T, Holz GG, Woods Jr VL, Cheng X.  (2012)  Isoform-specific antagonists of exchange proteins directly activated by cAMP..  Proc Natl Acad Sci USA,  109  (45): (18613-8).  [PMID:23091014]

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