CREB Inhibitor, 666-15-Calbiochem

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一般描述

A cell-permeable naphthol derivative that acts as a highly potent and selective inhibitor of cAMP response element-binding protein (CREB)-mediated gene transcription (IC50 = 81 nM by CREB RLuc reporter assay with transfected HEK 293T cells). Also shown to inhibit forskolin-stimulated transcription of Nurr1/NR4A2 (~ 50 nM). Diminishes CREB phosphorylation and reduces colony forming ability of wild-type AML cells. Inhibits the growth of cancer cells (GI₅₀= 46, 73, 310 and 470 nM for MDA-MB-468, MDA-MB-231, MCF-7, and A549, respectively) without affecting normal cells. Completely suppresses the growth of MDA-MB-468 xenografts in mice (~ 10 mg/kg, i.p., 5 days/week for 5 weeks).
A cell-permeable naphthol derivative that acts as a highly potent and selective inhibitor of cAMP response element-binding protein (CREB)-mediated gene transcription (IC50 = 81 nM by CREB RLuc reporter assay with transfected HEK 293T cells). Also shown to inhibit forskolin-stimulated transcription of Nurr1/NR4A2 (~ 50 nM). Diminishes CREB phosphorylation and reduces colony forming ability of wild-type AML cells. Inhibits the growth of cancer cells (GI₅₀= 46, 73, 310 and 470 nM for MDA-MB-468, MDA-MB-231, MCF-7, and A549, respectively) without affecting normal cells. Completely suppresses the growth of MDA-MB-468 xenografts in mice (~ 10 mg/kg, i.p., 5 days/week for 5 weeks).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

生化/生理作用

Cell permeable: yes
Primary Target
CREB
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

外形

Supplied as HCl salt

其他说明

Kang, X., et al. 2015.Nat. Cell. Biol.17,665.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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