Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (K d :8.6 μM), blocks the interaction between the KIX domain and the KID domain of CREB with IC 50 of 2.26 μM. Naphthol AS-E can be used for cancer research.
性状
Solid
IC50 & Target[1][2]
KIX-KID 2.26 μM (IC50)
体外研究(In Vitro)
CREB (cyclic AMP-response element-binding protein) is a downstream transcription factor of a multitude of signaling pathways emanating from receptor tyrosine kinases or G-protein coupled receptors.CREB can not be activated until it is phosphorylated at Ser133 and its subsequent binding to CREB-binding protein (CBP) through the kinase-inducible domain (KID) in CREB and KID-interacting (KIX) domain in CBP.In a cell-based CREB Renilla luciferase reporter assay, Naphthol AS-E inhibits CREB-mediated gene transcription with an IC50 of 2.29 μM. In HEK293T-based complementation assay, Naphthol AS-E dose-dependently inhibited Renilla luciferase activity with an IC50 of 2.9 μM by directly binding to CBPs KIX domain (Kd ~8.6 μM using a recombinant KIX).Naphthol AS-E exhibits low μM activity in inhibiting th
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Fuchun Xie, et al. Synthesis and Evaluation of an O-Aminated Naphthol AS-E as a Prodrug of CREB-mediated Gene Transcription Inhibition. Lett Org Chem. 2013 Jun;10(5):380-384.[2]. Bingbing X Li, et al. Discovery of a small-molecule inhibitor of the KIX-KID interaction. Chembiochem. 2009 Nov 23;10(17):2721-4.
溶解度数据
In Vitro: DMSO : 41.67 mg/mL (139.95 mM; Need ultrasonic)配制储备液