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Naphthol AS-E

CAS No. : 92-78-4

MCE 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 (K_d: 8.6 ?M)，阻断 KIX 域和 KID 域的相互作用 (IC₅₀: 2.26 ?M)。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 ?M. In HEK293T-based complementation assay, Naphthol AS-E?dose-dependently inhibited?Renilla?luciferase activity with an IC₅₀?of 2.9 ?M by directly binding to CBP's KIX domain (K_d ~8.6 ?M using a recombinant KIX).
Naphthol AS-E?exhibits low ?M 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?2.9?M, 2.81?M, 2.35?M and 1.46?M, respectively.
Naphthol AS-E (2.5 ?M-10 ?M; 48 hours) decreases the expression of anti-apoptotic protein Bcl-2. The expression of VEGF is also decreased.

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