Naphthol AS-E
Based on 1 Customer Validation
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.
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- Purity: 98.0%
- CAS No.: 92-78-4
- 화학식: C17H12ClNO2
- 분자량:297.74
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
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KIX-KID 2.26 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
2.9 μM
Compound: 1a
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Growth inhibition of human A549 cells after 72 hrs by MTT assay
Growth inhibition of human A549 cells after 72 hrs by MTT assay
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[PMID: 23102993] |
| A549 | IC50 |
2.9 μM
Compound: 1
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Growth inhibition of human A549 cells after 72 hrs by MTT assay
Growth inhibition of human A549 cells after 72 hrs by MTT assay
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[PMID: 25313320] |
| HEK-293T | IC50 |
2.29 μM
Compound: 1
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Inhibition of CREB (unknown origin) expressed in HEK293T cells assessed as reduction in CREB-mediated gene tanscription after 5 hrs by luciferase reporter gene assay
Inhibition of CREB (unknown origin) expressed in HEK293T cells assessed as reduction in CREB-mediated gene tanscription after 5 hrs by luciferase reporter gene assay
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[PMID: 25313320] |
| HEK-293T | IC50 |
2.29 μM
Compound: 1a
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Inhibition of CREB-mediated gene transcription in human HEK293T cells by renilla luciferase reporter assay
Inhibition of CREB-mediated gene transcription in human HEK293T cells by renilla luciferase reporter assay
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[PMID: 23102993] |
| HEK-293T | IC50 |
2.29 μM
Compound: Naphthol AS-E, 1
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Inhibition of CREB expressed in HEK293T cells assessed as inhibition of forskolin-stimulated CRE transcription incubated for 30 mins prior to forskolin-stimulation measured after 4.5 hrs by luciferase reporter gene assay
Inhibition of CREB expressed in HEK293T cells assessed as inhibition of forskolin-stimulated CRE transcription incubated for 30 mins prior to forskolin-stimulation measured after 4.5 hrs by luciferase reporter gene assay
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[PMID: 22458559] |
| MCF7 | GI50 |
2.81 μM
Compound: 1
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Growth inhibition of human MCF7 cells after 72 hrs by MTT assay
Growth inhibition of human MCF7 cells after 72 hrs by MTT assay
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[PMID: 25313320] |
| MCF7 | GI50 |
2.81 μM
Compound: 1a
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Growth inhibition of human MCF7 cells after 72 hrs by MTT assay
Growth inhibition of human MCF7 cells after 72 hrs by MTT assay
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[PMID: 23102993] |
| MDA-MB-231 | GI50 |
2.35 μM
Compound: 1
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Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay
Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay
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[PMID: 25313320] |
| MDA-MB-231 | GI50 |
2.35 μM
Compound: 1a
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Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay
Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay
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[PMID: 23102993] |
| MDA-MB-468 | GI50 |
1.46 μM
Compound: 1
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Growth inhibition of human MDA-MB-468 cells after 72 hrs by MTT assay
Growth inhibition of human MDA-MB-468 cells after 72 hrs by MTT assay
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[PMID: 25313320] |
| MDA-MB-468 | GI50 |
1.46 μM
Compound: 1a
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Growth inhibition of human MDA-MB-468 cells after 72 hrs by MTT assay
Growth inhibition of human MDA-MB-468 cells after 72 hrs by MTT assay
|
[PMID: 23102993] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 92-78-4
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Appearance Solid
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분자량 297.74
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화학식 C17H12ClNO2
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Color Light brown to brown
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SMILES
O=C(C1=C(O)C=C2C=CC=CC2=C1)NC3=CC=C(Cl)C=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
DMSO : 41.67 mg/mL (139.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3586 mL | 16.7932 mL | 33.5864 mL | 83.9659 mL |
| 5 mM | 0.6717 mL | 3.3586 mL | 6.7173 mL | 16.7932 mL | |
| 10 mM | 0.3359 mL | 1.6793 mL | 3.3586 mL | 8.3966 mL | |
| 15 mM | 0.2239 mL | 1.1195 mL | 2.2391 mL | 5.5977 mL | |
| 20 mM | 0.1679 mL | 0.8397 mL | 1.6793 mL | 4.1983 mL | |
| 25 mM | 0.1343 mL | 0.6717 mL | 1.3435 mL | 3.3586 mL | |
| 30 mM | 0.1120 mL | 0.5598 mL | 1.1195 mL | 2.7989 mL | |
| 40 mM | 0.0840 mL | 0.4198 mL | 0.8397 mL | 2.0991 mL | |
| 50 mM | 0.0672 mL | 0.3359 mL | 0.6717 mL | 1.6793 mL | |
| 60 mM | 0.0560 mL | 0.2799 mL | 0.5598 mL | 1.3994 mL | |
| 80 mM | 0.0420 mL | 0.2099 mL | 0.4198 mL | 1.0496 mL | |
| 100 mM | 0.0336 mL | 0.1679 mL | 0.3359 mL | 0.8397 mL |
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