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

CAS No.: 1357389-11-7

RGFP966 Catalog No. CSN17747

Synonyms: Rgfp966

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).

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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

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]
动物研究
剂量
Mice: 2 mg/kg - 10 mg/kg^[5] (i.p.); 10 mg/kg^[1] (s.c.), 25 mg/kg - 50 mg/kg^[6] (s.c.)

给药途径
i.p., s.c.
参考文献

动物研究
剂量	Mice: 2 mg/kg - 10 mg/kg^[5] (i.p.); 10 mg/kg^[1] (s.c.), 25 mg/kg - 50 mg/kg^[6] (s.c.)
给药途径	i.p., s.c.

[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.

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	1357389-11-7	储存条件	粉末 Sealed in dry,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

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