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KG-501

Cat. No. M10182

All AbMole products are for research use only, cannot be used for human consumption.

KG-501 Structure
Synonym:

Naphthol AS-E phosphate

Size Price Availability Quantity
1mg USD 30 In stock
5mg USD 55 In stock
10mg USD 80 In stock
50mg USD 177 In stock
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Biological Activity

KG-501 is a cAMP response element-binding protein (CREB) inhibitor with IC50 of 6.89 μM. KG-501 disrupts phospho (Ser-133) CREB binding to KIX with a Ki of ~90 μM, using concentrations of CREB that are within the linear range of the binding assay. Treatment of HEK293T cells with KG-501 also blocks induction of endogenous CREB target genes (NR4A2, αCG, c-fos, and RGS2) by forskolin, indicating that KG-501 likely exerts a general effect on CREB activity. KG-501 (10 μM) suppresses the expression of all of the IL-1β–induced CXC chemokine genes except CXCL8. For the protein level, KG-501 significantly suppresses IL-1β–induced CXCL5 protein secretion.

Chemical Information
Molecular Weight 377.72
Formula C17H13ClNO5P
CAS Number 18228-17-6
Solubility (25°C) DMSO 5 mg/mL warmed
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] RuiCai Gu, et al. Cell Physiol Biochem. Calcium/Calmodulin-Dependent Protein Kinase IV Mediates IFN-γ-Induced Immune Behaviors in Skeletal Muscle Cells

[2] Guofeng Wu, et al. Epilepsy Res. PKC/CREB pathway mediates the expressions of GABA A receptor subunits in cultured hippocampal neurons after low-Mg 2+ solution treatment

[3] Kaori Kubota, et al. Front Pharmacol. The Traditional Japanese Herbal Medicine Hachimijiogan Elicits Neurite Outgrowth Effects in PC12 Cells and Improves Cognitive in AD Model Rats via Phosphorylation of CREB

[4] Jong Woo Lee, et al. PLoS One. A Novel Small-Molecule Inhibitor Targeting CREB-CBP Complex Possesses Anti-Cancer Effects along with Cell Cycle Regulation, Autophagy Suppression and Endoplasmic Reticulum Stress

[5] Hongxia Sun, et al. Cancer Prev Res (Phila). Cyclic AMP-responsive element binding protein- and nuclear factor-kappaB-regulated CXC chemokine gene expression in lung carcinogenesis

[6] Jennifer L Best, et al. Proc Natl Acad Sci U S A. Identification of small-molecule antagonists that inhibit an activator: coactivator interaction

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Keywords: KG-501, Naphthol AS-E phosphate supplier, Epigenetic Reader Domain, inhibitors, activators

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