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CREB Inhibitor, 666-15-Calbiochem

产品编号:4083650
包装规格:10 MG
产品类别:进口试剂
品牌:Sigma-Aldrich
优惠价:立即咨询
产品价格
产品编号包装单位单价(元)国内现货国外库存询价单
408365010 MG2650
产品别名

CREB Inhibitor, 666-15-Calbiochem

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

基本信息
Empirical Formula【经验(实验)分子式】
C33H30ClN3O5 · xHCl
Molecular weight
584.06 (free base basis)
General description【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.
Biochem/physiol Actions【生化/生理作用】
Cell permeable: yes
Primary Target
CREB
Reversible: yes
Warning【警告】
Toxicity: Standard Handling (A)
Physical form【外形】
Supplied as HCl salt
Other Notes【其他说明】
Kang, X., et al. 2015. Nat. Cell. Biol.17, 665.
Legal Information【法律信息】
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
产品性质
Quality Level【质量水平】
100
Assay【测定】
≥98% (HPLC)
form【形式】
solid
manufacturer/tradename
Calbiochem®
storage condition【储存条件】
OK to freeze
desiccated (hygroscopic)
protect from light
color【颜色】
off-white
solubility【溶解性】
DMSO: 100 mg/mL
storage temp.【储存温度】
−20℃
packaging【包装】
Packaged under inert gas
安全信息
Storage Class Code【储存分类代码】
11 - Combustible Solids
WGK
WGK 3
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