Molecular Formula | C17H13ClNO5P |
Molar Mass | 377.72 |
Density | 1.567±0.06 g/cm3(Predicted) |
BRN | 6664478 |
pKa | 1.04±0.30(Predicted) |
Storage Condition | Keep in dark place,Inert atmosphere,2-8°C |
In vitro study | KG-501 inhibits (or partially inhibits) the induction of cAMP-related genes by preventing CREB:CBP interactions. KG-501 inhibited neurite outgrowth, synaptogenesis and decreased MAP2 neurons. |
In vivo study | KG-501 inhibited the expression of CREB, CCL2 and ERK phosphorylation while significantly reducing cAMP levels. CREB may help protect nerves against neuroinflammation through the cAMP/ERKadjustment pathway. KG-501 significantly promoted neurological function in the azoxymethane (AOM)-treated mouse model, reducing ERK phosphorylation levels and cAMP concentrations in the cortex. |
WGK Germany | 3 |
FLUKA BRAND F CODES | 8-10-21 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.647 ml | 13.237 ml | 26.475 ml |
5 mM | 0.529 ml | 2.647 ml | 5.295 ml |
10 mM | 0.265 ml | 1.324 ml | 2.647 ml |
5 mM | 0.053 ml | 0.265 ml | 0.529 ml |
Biological activity | KG-501 (2-naphthol-AS-E-phosphate) is a CREB inhibitor, which destroys the transcription of CREB (Ki = 10 μM) and CREB:CBP interaction (Ki = 50 μM). It can also destroy the binding of phosphorylated CREB(Ser-133) to KIX, Ki is about 90 μM. |
target | TargetValue CREB () |
Target | Value |
In vitro study | KG-501 inhibits (or partially inhibits) the induction of cAMP-related genes by preventing the CREB:CBP interaction. KG-501 inhibits neurite proliferation, synaptogenesis and reduces MAP2 nerve cells. |
in vivo study | KG-501 inhibited the expression of CREB, CCL2 and ERK phosphorylation, and significantly reduced the level of cAMP. CREB may help fight neuroinflammation through cAMP/ERKadjustment pathway, thus protecting nerves. KG-501 significantly promoted the neurological function of azomethane oxide (AOM)-treated mouse models and reduced the level of ERK phosphorylation and cAMP concentration in the cortex. |