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 ofKIX-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 withIC50of 2.26 μM. Naphthol AS-E can be used forcancerresearch. |
IC50& Target[1] | |
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 IC50of 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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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 | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 41.67 mg/mL(139.95 mM;Need ultrasonic) 配制储备液 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 |
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