| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
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| ln Vitro |
In several signaling pathways originating from G protein-coupled receptors or receptor tyrosine kinases, CREB (cyclic AMP response element binding protein) functions as a downstream transcription factor. Only phosphorylation at Ser133 may activate CREB, which then attaches to CREB-binding protein (CBP) via the KID (kinase-inducing domain) in CBP and the KID-interacting (KIX) domain in CREB. With an IC50 of 2.29 µM, naphthol AS-E suppresses CREB-mediated gene transcription in a cell-based CREB Renilla luciferase reporter experiment. Using recombinant KIX (Kd ~8.6 µM), naphthol AS-E directly binds to the KIX domain of CBP in a dose-dependent manner to block Renilla luciferase activity in a HEK293T-based complementation test. All of these cancer cells' growth was inhibited by naphthol AS-E with low µM activity, which is consistent with its cellular CREB inhibitory potency. Approximately 2.9μM, 2.81μM, 2.35μM, and 1.46μM are the average GI50 values of A549, MCF-7, MDA-MB-231, and MDA-MB-468, respectively. The anti-apoptotic protein Bcl-2's expression is decreased by naphthol AS-E (2.5 µM–10 µM; 48 hours). There is also a decrease in VEGF expression.
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|---|---|
| References |
| Molecular Formula |
C17H12CLNO2
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|---|---|
| Molecular Weight |
297.74
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| Exact Mass |
297.056
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| CAS # |
92-78-4
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| PubChem CID |
66720
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| Appearance |
Light brown to brown solid powder
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| Density |
1.399 g/cm3
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| Boiling Point |
416.5ºC at 760 mmHg
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| Melting Point |
255°C
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| Flash Point |
205.7ºC
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| Index of Refraction |
1.735
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| LogP |
4.524
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
368
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OHAXNCGNVGGWSO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H12ClNO2/c18-13-5-7-14(8-6-13)19-17(21)15-9-11-3-1-2-4-12(11)10-16(15)20/h1-10,20H,(H,19,21)
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| Chemical Name |
N-(4-chlorophenyl)-3-hydroxynaphthalene-2-carboxamide
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| Synonyms |
nAS E; nAS-E; Naphthol AS-E
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~41.67 mg/mL (~139.95 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.40 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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