
Naphthol AS-E
CAS No. 92-78-4
Naphthol AS-E( Naphthol AS-E | nAS-E | nAS E )
Catalog No. M16643 CAS No. 92-78-4
A cell-permeable inhibitor of the KIX-KID interaction and CREB-mediated gene transcription (IC50=2.26 uM).
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
100MG | 42 | Get Quote |
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200MG | 61 | Get Quote |
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500MG | 101 | Get Quote |
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Biological Information
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Product NameNaphthol AS-E
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NoteResearch use only, not for human use.
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Brief DescriptionA cell-permeable inhibitor of the KIX-KID interaction and CREB-mediated gene transcription (IC50=2.26 uM).
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DescriptionA 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.
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In VitroCREB (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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In Vivo——
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SynonymsNaphthol AS-E | nAS-E | nAS E
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PathwayNuclear Receptor/Transcription Factor
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TargetCREB/CBP
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RecptorCREB/CBP
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Research Area——
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Indication——
Chemical Information
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CAS Number92-78-4
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Formula Weight297.738
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Molecular FormulaC17H12ClNO2
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 41.67 mg/mL (139.95 mM)
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SMILESO=C(NC1=CC=C(Cl)C=C1)C2=C(O)C=C3C=CC=CC3=C2
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Chemical NameN-(4-chlorophenyl)-3-hydroxy-2-naphthamide
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Jiang M, et al. J Med Chem. 2012 Apr 26;55(8):4020-4.
2. Li BX, et al. Chembiochem. 2009 Nov 23;10(17):2721-4.
3. Best JL, et al. Proc Natl Acad Sci U S A. 2004 Dec 21;101(51):17622-7.
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