(E,E)-RGFP966

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Chemical Structure| 1396841-57-8 同义名 : RGFP966
CAS号 : 1396841-57-8
货号 : A411973
分子式 : C21H19FN4O
纯度 : 99%+
分子量 : 362.4
MDL号 : MFCD26960954
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(289.73 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 10%DMSO+30%PEG300+5%Tween80+55%water 2 mg/mL clear

生物活性
靶点

  • HDAC3

    HDAC3, IC50:80 nM
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
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.76mL

0.55mL

0.28mL

13.80mL

2.76mL

1.38mL

27.59mL

5.52mL

2.76mL
参考文献

[1]Malvaez M, McQuown SC, et al. HDAC3-selective inhibitor enhances extinction of cocaine-seeking behavior in a persistent manner. Proc Natl Acad Sci U S A. 2013 Feb 12;110(7):2647-52.

[2]Bieszczad KM, Bechay K, et al. Histone Deacetylase Inhibition via RGFP966 Releases the Brakes on Sensory Cortical Plasticity and the Specificity of Memory Formation. J Neurosci. 2015 Sep 23;35(38):13124-32.

[3]Matthews GM, Mehdipour P, et al. Functional-genetic dissection of HDAC dependencies in mouse lymphoid and myeloid malignancies. Blood. 2015 Nov 19;126(21):2392-403.

[4]Wagner FF, Weїwer M, et al. Small molecule inhibitors of zinc-dependent histone deacetylases. Neurotherapeutics. 2013 Oct;10(4):589-604.

[5]Jia H, Wang Y, et al. The Effects of Pharmacological Inhibition of Histone Deacetylase 3 (HDAC3) in Huntington's Disease Mice. PLoS One. 2016;11(3):e0152498.