1. Epigenetics
  2. Histone Acetyltransferase
    Epigenetic Reader Domain
  3. Naphthol AS-E

Naphthol AS-E 

Cat. No.: HY-104068 Purity: >98.0%
Handling Instructions

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 (Kd:8.6 µM), blocks the interaction between the KIX domain and the KID domain of CREB with IC50 of 2.26 µM. Naphthol AS-E can be used for cancer research.

For research use only. We do not sell to patients.

Naphthol AS-E Chemical Structure

Naphthol AS-E Chemical Structure

CAS No. : 92-78-4

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10 mM * 1 mL in DMSO Check price and availability
100 mg Check price and availability

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Description

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 (Kd:8.6 µM), blocks the interaction between the KIX domain and the KID domain of CREB with IC50 of 2.26 µM. Naphthol AS-E can be used for cancer research.

IC50 & Target[1]

KIX-KID

2.26 μM (IC50)

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

297.74

Formula

C₁₇H₁₂ClNO₂

CAS No.

92-78-4

SMILES

O=C(C1=C(O)C=C2C=CC=CC2=C1)NC3=CC=C(Cl)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (139.95 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3586 mL 16.7932 mL 33.5864 mL
5 mM 0.6717 mL 3.3586 mL 6.7173 mL
10 mM 0.3359 mL 1.6793 mL 3.3586 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (8.40 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.40 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Naphthol AS-EHistone AcetyltransferaseEpigenetic Reader DomainHATsHATKIX-KIDA549MCF-7MDA-MB-231cancerCBPCREBInhibitorinhibitorinhibit

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Naphthol AS-E
Cat. No.:
HY-104068
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