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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)

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Biological Information

  • Product Name
    Naphthol AS-E
  • Note
    Research use only, not for human use.
  • Brief Description
    A cell-permeable inhibitor of the KIX-KID interaction and CREB-mediated gene transcription (IC50=2.26 uM).
  • Description
    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.
  • 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 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.
  • In Vivo
    ——
  • Synonyms
    Naphthol AS-E | nAS-E | nAS E
  • Pathway
    Nuclear Receptor/Transcription Factor
  • Target
    CREB/CBP
  • Recptor
    CREB/CBP
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    92-78-4
  • Formula Weight
    297.738
  • Molecular Formula
    C17H12ClNO2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 41.67 mg/mL (139.95 mM)
  • SMILES
    O=C(NC1=CC=C(Cl)C=C1)C2=C(O)C=C3C=CC=CC3=C2
  • Chemical Name
    N-(4-chlorophenyl)-3-hydroxy-2-naphthamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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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