(E,E)-RGFP966 | RGFP966 | HDAC | AmBeed-信号通路专用抑制剂

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(E,E)-RGFP966 {[allProObj[0].p_purity_real_show]}

货号：A411973 同义名： RGFP966

(E,E)-RGFP966 是一种选择性的 HDAC3 抑制剂，对 HDAC3 具有高亲和力，IC50 值为 80 nM。RGFP966 具有神经保护和抗抑郁作用，可用于神经退行性疾病和精神疾病的研究。

(E,E)-RGFP966 化学结构
CAS号：1396841-57-8

(E,E)-RGFP966 3D分子结构
CAS号：1396841-57-8

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(E,E)-RGFP966 纯度/质量文件产品仅供科研

货号：A411973 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

组蛋白去乙酰化酶亚型比较

产品名称	HD1 ↓ ↑	HD2 ↓ ↑	HDAC ↓ ↑	HDAC1 ↓ ↑	HDAC10 ↓ ↑	HDAC11 ↓ ↑	HDAC2 ↓ ↑	HDAC3 ↓ ↑	HDAC4 ↓ ↑	HDAC5 ↓ ↑	HDAC6 ↓ ↑	HDAC7 ↓ ↑	HDAC8 ↓ ↑	HDAC9 ↓ ↑	其他靶点	纯度
Givinostat HCl monohydrate	++++ HD1-A, IC50: 16 nM HD1-B, IC50: 7.5 nM	+++ HD2, IC50: 10 nM														99%+
MC1568	++ HD1-A (Maize), IC50: 100 nM HD1-B (Maize), IC50: 3.4 μM															96%
Trichostatin A			++++ HDAC, IC50: ~1.8 nM													99%+
Scriptaid			✔													99%+
Valproic acid sodium			✔												Autophagy	97%
AR-42			+++ HDAC, IC50: 30 nM													99%+
Dacinostat			+++ HDAC, IC50: 32 nM													98+%
CUDC-101			++++ HDAC, IC50: 4.4 nM	++++ HDAC1, IC50: 4.5 nM	+++ HDAC10, IC50: 26.1 nM		+++ HDAC2, IC50: 12.6 nM	++++ HDAC3, IC50: 9.1 nM	+++ HDAC4, IC50: 13.2 nM	+++ HDAC5, IC50: 11.4 nM	++++ HDAC6, IC50: 5.1 nM	+ HDAC7, IC50: 373 nM	++ HDAC8, IC50: 79.8 nM	++ HDAC9, IC50: 67.2 nM	EGFR,HER2	99%+
M344			++ HDAC, IC50: 100 nM													99%+
Splitomicin			+ Sir2p, IC50: 60 μM													95%
Panobinostat			++++ HDAC (Reh cells), IC50: 20 nM HDAC (MOLT-4 cells), IC50: 5 nM													98%
Sodium 4-Phenylbutyrate			✔													98%
Vorinostat			+++ HDAC, IC50: ~10 nM													98%
Curcumin			✔												Nrf2,NF-κB	98%
Belinostat			+++ HDAC, IC50: 27 nM													98%
RG-2833				++ HDAC1, Ki: 32 nM				++ HDAC3, Ki: 5 nM								98%
Valproic acid				+ HDAC1, IC50: 0.4 mM												98%
BG45				+ HDAC1, IC50: 2 μM			+ HDAC2, IC50: 2.2 μM	+ HDAC3, IC50: 289 nM								99%+
Entinostat				+ HDAC1, IC50: 0.51 μM				+ HDAC3, IC50: 1.7 μM								98%
Resminostat				+++ HDAC1, IC50: 42.5 nM				++ HDAC3, IC50: 50.1 nM			++ HDAC6, IC50: 71.8 nM					98+%
Romidepsin				+++ HDAC1, IC50: 36 nM			+++ HDAC2, IC50: 47 nM									99%+
Parthenolide				✔											p53,NF-κB	97% HPLC
Tacedinaline				+ HDAC1, IC50: 0.9 μM			+ HDAC2, IC50: 0.9 μM	+ HDAC3, IC50: 1.2 μM								98%
Mocetinostat				++ HDAC1, IC50: 0.15 μM		+ HDAC11, IC50: 0.59 μM	+ HDAC2, IC50: 0.29 μM	+ HDAC3, IC50: 1.66 μM								98%
WT-161				++++ HDAC1, IC50: 8.35 nM			+++ HDAC2, IC50: 15.4 nM				++++ HDAC6, IC50: 0.4 nM					99%+
Fimepinostat				++++ HDAC1, IC50: 1.7 nM	++++ HDAC10, IC50: 2.8 nM	++++ HDAC11, IC50: 5.4 nM	++++ HDAC2, IC50: 5.0 nM	++++ HDAC3, IC50: 1.8 nM			+++ HDAC6, IC50: 27 nM					99%+
Tucidinostat				++ HDAC1, IC50: 95 nM	++ HDAC10, IC50: 78 nM		++ HDAC2, IC50: 160 nM	++ HDAC3, IC50: 67 nM								99%+
Santacruzamate A							++++ HDAC2, IC50: 119 pM									99%+
(E,E)-RGFP966								++ HDAC3, IC50: 80 nM								99%+
LMK-235									+++ HDAC4, IC50: 11.9 nM	++++ HDAC5, IC50: 4.2 nM						99%+
Tasquinimod									✔							99%+
CAY10603											++++ HDAC6, IC50: 2 pM					98%
Tubastatin A											+++ HDAC6, IC50: 15 nM					98%
Tubacin											++++ HDAC6, IC50: 4 nM					99%+
ACY-738											++++ HDAC6, IC50: 1.7 nM					99%+
Nexturastat A											++++ HDAC6, IC50: 5 nM					99%+
BRD73954											+++ HDAC6, IC50: 36 nM		++ HDAC8, IC50: 120 nM			98%
Tubastatin A HCl											+++ HDAC6, IC50: 15 nM		+ HDAC8, IC50: 854 nM			98%
PCI-34051													+++ HDAC8, IC50: 10 nM			99%+
Ricolinostat				++ HDAC1, IC50: 58 nM			++ HDAC2, IC50: 48 nM	++ HDAC3, IC50: 51 nM			++++ HDAC6, IC50: 4.7 nM		++ HDAC8, IC50: 100 nM			99%+
Droxinostat								+ HDAC3, IC50: 16.9 μM			+ HDAC6, IC50: 2.47 μM		+ HDAC8, IC50: 1.46 μM			99%+
Abexinostat				++++ HDAC1, Ki: 7 nM	+++ HDAC10, IC50: 24 nM		+++ HDAC2, Ki: 19 nM	++++ HDAC3/SMRT, Ki: 8.2 nM			+++ HDAC6, Ki: 17 nM		+ HDAC8, IC50: 280 nM			98%+
Citarinostat				+++ HDAC1, IC50: 35 nM			+++ HDAC2, IC50: 45 nM	+++ HDAC3, IC50: 46 nM			++++ HDAC6, IC50: 2.6 nM		++ HDAC8, IC50: 137 nM			99%+
HPOB				+ HDAC1, IC50: 2.9 μM	+ HDAC10, IC50: 3.0 μM		+ HDAC2, IC50: 4.4 μM	+ HDAC3, IC50: 1.7 μM			++ HDAC6, IC50: 56 nM		+ HDAC8, IC50: 2.8 μM			97%
Quisinostat 2HCl				++++ HDAC1, IC50: 0.11 nM	++++ HDAC10, IC50: 0.46 nM	++++ HDAC11, IC50: 0.37 nM	++++ HDAC2, IC50: 0.33 nM	++++ HDAC3, IC50: 4.86 nM	++++ HDAC4, IC50: 0.64 nM	++++ HDAC5, IC50: 3.69 nM			++++ HDAC8, IC50: 4.26 nM			99+%
Domatinostat				+ HDAC1, IC50: 1.20 μM	+ HDAC10, IC50: 21 μM	+ HDAC11, IC50: 9.7 μM	+ HDAC2, IC50: 1.12 μM	+ HDAC3, IC50: 0.57 μM		+ HDAC5, IC50: 11.3 μM				+ HDAC9, IC50: 50 μM		99%+
TMP269									++ HDAC4, IC50: 157 nM	++ HDAC5, IC50: 97 nM		+++ HDAC7, IC50: 43 nM		+++ HDAC9, IC50: 23 nM		99%+
Pracinostat				++ HDAC1, IC50: 49 nM	+++ HDAC10, IC50: 40 nM	++ HDAC11, IC50: 93 nM	++ HDAC2, IC50: 96 nM	+++ HDAC3, IC50: 43 nM	++ HDAC4, IC50: 56 nM	+++ HDAC5, IC50: 47 nM	+ HDAC6, IC50: 1.008 μM	++ HDAC7, IC50: 137 nM	++ HDAC8, IC50: 140 nM	++ HDAC9, IC50: 70 nM		99%+
TMP195									++ HDAC4, Ki: 59 nM	++ HDAC5, Ki: 60 nM		+++ HDAC7, Ki: 26 nM		+++ HDAC9, Ki: 15 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

(E,E)-RGFP966 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]

(E,E)-RGFP966 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
HH and Hut78 cells	10 μM	Proliferation assay	0, 24, 48, 72 h	Both cell lines were sensitive to treatment with 10 μM 966. However, Hut78 cells exhibited a greater sensitivity than HH cells.	23894374

(E,E)-RGFP966 动物研究

Dose	Mice: min = 10 mg/kg^[1], max = 25 mg/kg^[5]
Administration	s.c., i.p.

(E,E)-RGFP966 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.

(E,E)-RGFP966 实验方案

计算器

存储液制备

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

(E,E)-RGFP966 技术信息

CAS号	1396841-57-8
分子式	C₂₁H₁₉FN₄O
分子量	362.4

别名	RGFP966
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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

(E,E)-RGFP966 {[allProObj[0].p_purity_real_show]}

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(E,E)-RGFP966 生物活性

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(E,E)-RGFP966 动物研究

(E,E)-RGFP966 参考文献

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全球学术期刊中引用的产品

(E,E)-RGFP966 质控信息

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(E,E)-RGFP966 细胞研究

(E,E)-RGFP966 动物研究

(E,E)-RGFP966 参考文献

(E,E)-RGFP966 实验方案

(E,E)-RGFP966 技术信息

最近浏览的产品

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