Home Epigenetics Epigenetic Reader Domain inhibitor KG-501 For research use only.

KG-501

Synonyms: 2-naphthol-AS-E-phosphate

KG-501 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 Chemical Structure

KG-501 Chemical Structure

CAS: 18228-17-6

Selleck's KG-501 has been cited by 15 publications

Purity & Quality Control

Batch: S840901 DMSO] 20 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.81%
99.81

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Biological Activity

Description KG-501 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
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-CREB 15585582
In Vivo
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].
Animal Research Animal Models Murine azoxymethane (AOM) model of hepatic encephalopathy (Adult male C57BL/6 mice)
Dosages 10, 20, or 50 μM
Administration intracerebroventricular infusion

Chemical Information & Solubility

Molecular Weight 377.72 Formula

C17H13ClNO5P
CAS No. 18228-17-6 SDF --
Smiles C1=CC=C2C=C(C(=CC2=C1)C(=O)NC3=CC=C(C=C3)Cl)OP(=O)(O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 20 mg/mL ( (52.94 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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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