Name | Naphthol AS-E phosphate |
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Synonyms |
naphthol as-e phosphate
KG-501 |
Description | KG-501 is a CREB inhibitor, with an IC50 of 6.89 μM. |
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Related Catalog | |
Target |
IC50: 6.89 μM (CREB)[1]. |
In Vitro | KG-501, which directly targets the KIX domain of CBP, results in a disrupted CREB-CBP complex, inhibits CREB-target gene induction, and inhibits IL-1β-mediated angiogenic activity in NSCLC[1]. 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[2]. KG-501 can also inhibit NF-κB transcription activity because NF-κB also uses CBP as a cofactor to regulate gene expression. The migration of HUVECs induced by CM from A549 cells treated with IL-1β plus 10 μM of KG-501 is significantly lower than that induced by CM from A549 cells treated with IL-1β alone. At 10 μM, KG-501 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. Similar effects of KG-501 are also observed in the H1734 cell line[3]. |
References |
Density | 1.567g/cm3 |
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Molecular Formula | C17H13ClNO5P |
Molecular Weight | 377.71600 |
Exact Mass | 377.02200 |
PSA | 105.67000 |
LogP | 4.29000 |
Index of Refraction | 1.723 |
Storage condition | -20℃ |
Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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RIDADR | NONH for all modes of transport |
WGK Germany | 3 |