Naphthol AS-E
目录号: PL13453 纯度: ≥98.0%
CAS No. :92-78-4
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中文名称
Naphthol AS-E
中文别名
色酚AS-E;纳夫妥AS-E;C.I.冰染偶合组分10;4'-氯-3-羟基-2-萘苯胺;4 -氯-3-羟基-2-萘苯胺;4'-Chloro-3-hydroxy-2-naphthanilide 4'-氯-3-羟基-2-萘苯胺;4''-氯-3-羟基-2-萘苯胺;萘酚AS-E;2-羟基-N-(4氯基苯基)-3-萘甲酰胺;N-(3-羟基-2-萘甲酰基)对氯苯胺;冰染偶合组分 10;色酚 AS-E
英文名称
Naphthol AS-E
英文别名
Naphthol AS-E;C.I.Azoic Coupling Component 10;4'-Chloro-3-hydroxy-2-naphthanilide;1-(4-Pyridyl)Ethylamine;N-(4-chlorophenyl)-3-hydroxynaphthalene-2-carboxamide;3-Hydroxy-[2]naphthoesaeure-(4-chlor-anilid);3-hydroxy-[2]naphthoic acid-(4-chloro-anilide);3-hydroxy-naphthalene-2-carboxylic acid 4-chloro-anilide;Amanil Naphthol AS-E;Cibanaphthol RC;Daito Grounder E;Naphtanilide E;Naphtazol E;Naphtoelan E;Sanatol E;Azoic Coupling Component 10;N-(4-Chlorophenyl)-3-hydroxy-2-naphthamide;C.I. 37510;C.I. Azoic Coupling Component 10;2-Naphthalenecarboxamide, N-(4-chlorophenyl)-3-hydroxy-;Tulathol AS-E;Amarthol AS-E;Acna Naphthol PC;Naphthol ACNA PC;Hiltonaphthol AS-E;Naphtol AS-E Supra;C.I. 375;2-Naphthanilide, 4′-chloro-3-hydroxy- (6CI, 7CI, 8CI);N-(4-Chlorophenyl)-3-hydroxy-2-naphthalenecarboxamide (ACI);3-Hydroxy-4′-chloro-2-naphthanilide;4′-Chloro-3-hydroxy-2-naphthanilide;Anarthol AS-E;Conazoic AO;Dycosthol AS-E;Kako Grounder E;Kiwa Grounder E;Naftol AS-E;Napthol ASE;NSC 50684;Red RC Base
Cas No.
92-78-4
分子式
C17H12ClNO2
分子量
297.74
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
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 (K d :8.6 μM), blocks the interaction between the KIX domain and the KID domain of CREB with IC 50 of 2.26 μM. Naphthol AS-E can be used for cancer research.
性状
Solid
IC50 & Target[1][2]
KIX-KID 2.26 μM (IC50)
体外研究(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 CBPs KIX domain (Kd ~8.6 μM using a recombinant KIX).
Naphthol AS-E exhibits low μM activity in inhibiting th
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
[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.
溶解度数据
In Vitro: DMSO : 41.67 mg/mL (139.95 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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