Naphthol AS-E

Research use only, not for human use.

A cell-permeable inhibitor of the KIX-KID interaction and CREB-mediated gene transcription (IC50=2.26 uM).

A cell-permeable inhibitor of the KIX-KID interaction and CREB-mediated gene transcription (IC50=2.26 uM); the first KIX-binding small molecule to inhibit CREB-dependent gene transcription in living cells with IC50 in the low-uM range and a novel template for inhibiting protein-protein interactions.

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 CBP's KIX domain (Kd ~8.6 μM using a recombinant KIX).Naphthol AS-E?exhibits low μM activity in inhibiting the proliferation of all these cancer cells, which is consistent with its cellular CREB inhibition potency. The average GI50?values for A549, MCF-7, MDA-MB-231 and MDA-MB-468 are approximately?2.9μM, 2.81μM, 2.35μM and 1.46μM, respectively.Naphthol AS-E (2.5 μM-10 μM; 48 hours) decreases the expression of anti-apoptotic protein Bcl-2. The expression of VEGF is also decreased.

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Naphthol AS-E | nAS-E | nAS E

Nuclear Receptor/Transcription Factor

CREB/CBP

CREB/CBP

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92-78-4

297.738

C17H12ClNO2

>98% (HPLC)

In Vitro:?DMSO : 41.67 mg/mL (139.95 mM)

O=C(NC1=CC=C(Cl)C=C1)C2=C(O)C=C3C=CC=CC3=C2

N-(4-chlorophenyl)-3-hydroxy-2-naphthamide

(-20℃)

With Ice Pack

≥ 2 years