KG-501 (2-naphthol-AS-E-phosphate)

Catalog No.S8409

For research use only.

KG-501 (2-naphthol-AS-E-phosphate) is a cAMP response element-binding protein (CREB) inhibitor that disrupts CREB-dependent transcription (Ki = 10 μM) and CREB:CBP interaction (Ki = 50 μM). It also disrupts phospho (Ser-133) CREB binding to KIX with a Ki of ≈90 μM, using concentrations of CREB that were within the linear range of the binding assay.

KG-501 (2-naphthol-AS-E-phosphate) Chemical Structure

CAS No. 18228-17-6

Selleck's KG-501 (2-naphthol-AS-E-phosphate) has been cited by 13 publications

Purity & Quality Control

Choose Selective Epigenetic Reader Domain Inhibitors

Biological Activity

Description KG-501 (2-naphthol-AS-E-phosphate) is a cAMP response element-binding protein (CREB) inhibitor that disrupts CREB-dependent transcription (Ki = 10 μM) and CREB:CBP interaction (Ki = 50 μM). It also disrupts phospho (Ser-133) CREB binding to KIX with a Ki of ≈90 μM, using concentrations of CREB that were within the linear range of the binding assay.
Targets
CREB [1]
()
In vitro

KG-501 inhibits induction of cAMP-responsive genes, at least in part, by blocking the CREB:CBP interaction[1]. The inhibition of the CREB pathway using KG-501, induces an inhibition of neurite outgrowth and synaptogenesis, as well as a decrease of MAP2+ neuronal cells[2].

Assay
Methods Test Index PMID
Western blot p-CREB 15585582
In vivo

KG-501 inhibits CREB, CCL2 expression and ERK phosphorylation, also significantly lowers the cAMP level. CREB might contribute to the neuroprotection opposed neuroinflammation through cAMP/ERK adjustment pathway. KG-501 significantly promots the neurological outcomes of AOM-treated mice, reduces phosphorylation of ERK and the concentration of cAMP in cortex[3].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: HEK293T cells
  • Concentrations: 5, 10, 25 μM
  • Incubation Time: 20 min
  • Method:

    EVX-1 luciferase reporter plasmid was transfected into HEK293T cells. At 24 h posttransfection, cells were pretreated with the indicated amount of KG-501 or DMSO vehicle for 20 min followed by coincubation with forskolin or DMSO. Cells were harvested at 4 h, and luciferase activity was measured.

Animal Research:

[3]

  • Animal Models: Murine azoxymethane (AOM) model of hepatic encephalopathy (Adult male C57BL/6 mice)
  • Dosages: 10, 20, or 50 μM
  • Administration: intracerebroventricular infusion

Solubility (25°C)

In vitro

DMSO 20 mg/mL
(52.94 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 377.72
Formula

C17H13ClNO5P

CAS No. 18228-17-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C2C=C(C(=CC2=C1)C(=O)NC3=CC=C(C=C3)Cl)OP(=O)(O)O

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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