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Crebinostat

目录号 : GC70432

Crebinostat是一种强效的组蛋白脱乙酰酶(HDAC)抑制剂,对HDAC1、HDAC2、HDAC3和HDAC6的IC50值分别为0.7 nM、1.0 nM、2.0 nM和9.3 nM。

Crebinostat Chemical Structure

Cas No.:1092061-61-4

规格 价格 库存 购买数量
1 mg
¥1,890.00
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5 mg
¥4,680.00
现货
10 mg
¥6,570.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, 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 gene Egr1. 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.

Crebinostat (1 μM; 24 h) induces acetylation of AcH4K12 and AcH3K9 in mouse primary neuronal cells[1].
Crebinostat (1 μM; 24 h) downregulates Mapt mRNA expression, and upregulates Hspa1b (Hsp70) and Bdnf mRNA 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].

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].

References:
[1]. Fass DM, et al. Crebinostat: a novel cognitive enhancer that inhibits histone deacetylase activity and modulates chromatin-mediated neuroplasticity. Neuropharmacology. 2013 Jan;64:81-96.

Chemical Properties

Cas No. 1092061-61-4 SDF
分子式 C20H23N3O3 分子量 353.41
溶解度 DMSO : 100 mg/mL (282.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) 储存条件 -20°C
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1 mg 5 mg 10 mg
1 mM 2.8296 mL 14.1479 mL 28.2957 mL
5 mM 0.5659 mL 2.8296 mL 5.6591 mL
10 mM 0.283 mL 1.4148 mL 2.8296 mL
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