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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.
| 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 |
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