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Merck
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Key Documents

5.38341

Sigma-Aldrich

666-15

≥98% (HPLC), solid, CREB inhibitor, Calbiochem®

別名:

CREB Inhibitor, 666-15, 3-(3-Aminopropoxy)-N-(2-((3-((4-chloro-2-hydroxyphenyl)carbamoyl)naphthalen-2-yl)oxy)ethyl)-2-naphthamide, HCl, CBP-CREB Interaction Inhibitor II, 666-15

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About This Item

実験式(ヒル表記法):
C33H30ClN3O5 · xHCl
分子量:
584.06 (free base basis)
UNSPSCコード:
12352200
NACRES:
NA.77

product name

CREB Inhibitor, 666-15,

アッセイ

≥98% (HPLC)

品質水準

形状

solid

メーカー/製品名

Calbiochem®

保管条件

OK to freeze
desiccated (hygroscopic)
protect from light

off-white

溶解性

DMSO: 100 mg/mL

保管温度

−20°C

詳細

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.

生物化学的/生理学的作用

Cell permeable: yes
Primary Target
CREB
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

物理的形状

Supplied as HCl salt

その他情報

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

法的情報

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

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable


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