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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
92-78-4
- 规格：
10 mM * 1 mL/50 mg/100 mg/500 mg/1 g
| 规格： | 10 mM * 1 mL | 产品价格： | ￥660.0 |
|---|---|---|---|
| 规格： | 50 mg | 产品价格： | ￥225.0 |
| 规格： | 100 mg | 产品价格： | ￥360.0 |
| 规格： | 500 mg | 产品价格： | ￥860.0 |
| 规格： | 1 g | 产品价格： | ￥1200.0 |
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Naphthol AS-E
CAS No. : 92-78-4
MCE 国际站：Naphthol AS-E
产品活性：Naphthol AS-E 是有效的，具有细胞渗透性的 KIX-KID 相互作用的抑制剂。Naphthol AS-E 直接结合 CBP 的 KIX 域 (Kd: 8.6 µM)，阻断 KIX 域和 KID 域的相互作用 (IC50: 2.26 µM)。Naphthol AS-E 可用于癌症研究。
研究领域：Epigenetics
作用靶点：Histone Acetyltransferase | Epigenetic Reader Domain
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.
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文献和实验27 4.24 3.65 3.31 3.08 2.92 2.80 2.71 2.63 2.57 2.47 2.36 2.25 2.13 2.00 1.85 27 28 4.22 3.63 3.29 3.06 2.90 2.78 2.69 2.61 2.55 2.45 2.34 2.23 2.11 1.98 1.83 28 29 4.20 3.61 3.27 3.04 2.88 2.76 2.67 2.59 2.53 2.43 2.32 2.21 2.09 1.96 1.81 29
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2.13 2.07 2.03 1.95 1.89 1.85 1.81 1.78 50 60 4.00 3.15 2.76 2.53 2.37 2.25 2.17 2.10 2.04 1.99 1.92 1.86 1.82 1.78 1.75 60 80 3.96 3.11 2.72 2.49 2.33 2.21 2.13 2.06 2.00 1.95 1.88 1.82 1.77 1.73 1.70 80 100 3.94 3.09 2.70 2.46 2.31 2.19 2.10 2.03
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