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Crebinostat
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Crebinostat图片
CAS NO:1092061-61-4
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
Crebinostat 是一种有效的组蛋白去乙酰化酶 (HDAC)抑制剂，对 HDAC1、HDAC2、HDAC3 和 HDAC6 的IC50分别为 0.7 nM、1.0 nM、2.0 nM 和 9.3 nM。Crebinostat 可诱导组蛋白 H3 和组蛋白 H4 乙酰化，并增强 cAMP 反应元件结合蛋白 (CREB) 靶基因Egr1的表达。Crebinostat 可增加在体外神经元的突触蛋白 1 斑点沿树突 (synapsin-1 punctae along dendrites) 的密度。Crebinostat 可调节染色质介导的神经可塑性，增强小鼠的记忆。
生物活性

Crebinostat is a potenthistone deacetylase (HDAC)inhibitor withIC50values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM forHDAC1,HDAC2,HDAC3andHDAC6, respectively. Crebinostat potently induces acetylation of both histone H3 and histone H4 as well as enhances the expression of the cAMP response element-binding protein (CREB) target geneEgr1. Crebinostat increases the density of synapsin-1 punctae along dendrites in cultured neurons. Crebinostat can modulate chromatin-mediated neuroplasticity and exhibits enhanced memory in mice[1].

IC50& Target[1]

HDAC1

0.7 nM (IC50)

HDAC2

1.0 nM (IC50)

HDAC3

2.0 nM (IC50)

HDAC6

9.3 nM (IC50)

体外研究
(In Vitro)

Crebinostat (1 μM; 24 h) induces acetylation of AcH4K12 and AcH3K9 in mouse primary neuronal cells[1].
Crebinostat (1 μM; 24 h) downregulatesMaptmRNA expression, and upregulatesHspa1b(Hsp70) andBdnfmRNA expression in mouse primary cultured neurons[1].
Crebinostat (1 μM; 24 h) increases histone acetylation and synapsin I punctae along dendrites in primary cultured neurons[1].

Western Blot Analysis[1]

Cell Line:Mouse primary neuronal cells (dissociated from E17 embryonic mouse forebrain)
Concentration:1 μM
Incubation Time:24 h
Result:Induced robust acetylation of AcH4K12 and AcH3K9 in a dose dependent manner with EC50s of 0.29 μM and 0.18 μM.
体内研究
(In Vivo)

Crebinostat (25 mg/kg; IP; for 10 days) enhances memory of contextual fear conditioning in mice; induces an increase in total hippocampal acetylation of H4K12 and H3K9[1].

Animal Model:Male C57BL/6J mice (9-10 weeks)[1]
Dosage:25 mg/kg
Administration:IP; alternate daily between left and right sides of the abdomen, for 10 days
Result:Enhanced memory of contextual fear conditioning in mice; induced a trend towards an increase in total hippocampal acetylation of both H4K12 and H3K9.
分子量

353.41

Formula

C20H23N3O3

CAS 号

1092061-61-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.