|(E)-N-(2-氨基-4-氟苯基)-3-(1-肉桂基-1H-吡唑基-4-基)丙烯酰胺|CsnPharm

CAS No.: 1396841-57-8

(E)-N-(2-Amino-4-fluorophenyl)-3-(1-cinnamyl-1H-pyrazol-4-yl)acrylamide Catalog No. CSN18796

Synonyms: RGFP966 Racemate

RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HDAC3

IC50:0.08μM
描述HDAC3, the most highly expressed class I HDAC in the brain, is a key negative regulator of gene expression required for long-term memory formation. RGFP966 is speciﬁc inhibitor of HDAC3 with an IC50 of 0.08 μM and no effective inhibition of any other HDAC at concentrations up to 15 μM (measured by enzymatic activity of recombinant human HDACs). A series of function in memory of RGFP966 has been done. 10 mg/kg RGFP966 subcutaneously posttreatment cause increased H4K8Ac, a site regulated by HDAC3 activity in the brain, and H3K14Ac, correlating with learning, in infralimbic cortex of mice at 1 h after the ﬁrst extinction session of cocaine-CPP^[1]. A posttraining injection of RGPF966 (10 mg/kg, s.c.) following the daily training session in rat can alter the formation of auditory memory by enabling more acoustic information to become encoded into memory and affect the cortical plasticity^[2]. A study shows the function of RGFP966 in lymphoid and myeloid malignancies. Incubation with RGFP966 (<1uM,48h) significantly slowed down the proliferation of Eu-Myc lymphoma cells and increased maturation of APL cells, without induction of apoptosis^[3].
作用机制The ortho-aminoanilide structure of RGFP966 is the zinc-binding moiety.^[4]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
APL cells	≤2 μM	Function assay	48 h	RGFP966 did not induce apoptosis in APL cells but did reduce clonogenicity and increased maturation.	26447190
Em-Myc lymphoma cells	≤1 μM	Function assay	48 h	Cell proliferated significantly more slowly than vehicle-treated controls in the presence or absence of pro-survival BCL-2 overexpression	26447190
HH	10 μM	Function assay	24 h	increases the acetylation at H3K9/K14, H3K27, and H4K5	23894374

更多
动物研究
剂量
Mice: min = 10 mg/kg^[1], max = 25 mg/kg^[5]

给药途径
s.c., i.p.
参考文献

动物研究
剂量	Mice: min = 10 mg/kg^[1], max = 25 mg/kg^[5]
给药途径	s.c., i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7594 mL
- 13.7969 mL
- 27.5938 mL
- 5 mM
- 0.5519 mL
- 2.7594 mL
- 5.5188 mL
- 10 mM
- 0.2759 mL
- 1.3797 mL
- 2.7594 mL

技术信息

CAS号

1396841-57-8

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H19FN4O

运输

蓝冰

分子量

362.40

别名

RGFP966 Racemate

溶解度

DMSO	68.0 mg/mL (187.6 mM)
Water	insoluble

动物实验配方

10%DMSO+30%PEG300+5%Tween80+55%water

2 mg/mL

clear

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(E)-N-(2-Amino-4-fluorophenyl)-3-(1-cinnamyl-1H-pyrazol-4-yl)acrylamide Catalog No. CSN18796

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