MC1568
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
MC1568，(Aryloxopropenyl)pyrrolyl hydroxyamide的衍生物，是一种新型有效的和特异性的II类组蛋白去乙酰化酶（HDAC）抑制剂，对玉米的II类HDAC具有强烈的抑制效应，IC50值为22 μM。II类HDAC包括两个子类：IIa（HDAC4、HDAC5、HDAC6、HDAC7和HDAC9）和Ⅱb（HDAC6和HDAC10）。据报道，在培养的肌细胞中，MC1568通过三种可能的机制，组织选择性地抑制HDAC和肌肉发生，包括减少肌细胞增强因子2D的表达，稳定HDAC-HDAC3-MEF2D复合体和抑制分化诱导的MEF2D乙酰化。而且，MC1568能够干扰RAR和PPARγ介导的分化诱导的信号通路。
参考文献：
Mai A, Massa S, Pezzi R, Simeoni S, Rotili D, Nebbioso A, Scognamiglio A, Altucci L, Loidl P, Brosch G. Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides. J Med Chem. 2005 May 5;48(9):3344-53.
Nebbioso A, Dell'Aversana C, Bugge A, Sarno R, Valente S, Rotili D, Manzo F, Teti D, Mandrup S, Ciana P, Maggi A, Mai A, Gronemeyer H, Altucci L. HDACs class II-selective inhibition alters nuclear receptor-dependent differentiation. J Mol Endocrinol. 2010 Oct;45(4):219-28. doi: 10.1677/JME-10-0043. Epub 2010 Jul 16.
Nebbioso A, Manzo F, Miceli M, Conte M, Manente L, Baldi A, De Luca A, Rotili D, Valente S, Mai A, Usiello A, Gronemeyer H, Altucci L. Selective class II HDAC inhibitors impair myogenesis by modulating the stability and activity of HDAC-MEF2 complexes. EMBO Rep. 2009 Jul;10(7):776-82. doi: 10.1038/embor.2009.88. Epub 2009 Jun 5.
- 1.Hari Prasad, Rajini Rao. "The Amyloid Clearance Defect in ApoE4 Astrocytes is Corrected by Epigenetic Restoration of NHE6." bioRxiv. 2018.January. 4
- 2.Griffin EA Jr, Melas PA, et al. "Prior alcohol use enhances vulnerability to compulsive cocaine self-administration by promoting degradation of HDAC4 and HDAC5." Sci Adv. 2017 Nov 1;3(11):e1701682. PMID:29109977
- 3.Ha, Soon-Duck, et al. "Inhibition of IL-1β Expression by Anthrax Lethal Toxin is Reversed by HDAC8 Inhibition in Murine Macrophages." Journal of Biological Chemistry (2016): jbc-M115. PMID:26912657
| Storage | Store at -20°C |
| M.Wt | 314.31 |
| Cas No. | 852475-26-4 |
| Formula | C17H15FN2O3 |
| Synonyms | MC 1568, MC-1568 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥15.7 mg/mL in DMSO |
| Chemical Name | (E)-3-[4-[(E)-3-(3-fluorophenyl)-3-oxoprop-1-enyl]-1-methylpyrrol-2-yl]-N-hydroxyprop-2-enamide |
| SDF | Download SDF |
| Canonical SMILES | CN1C=C(C=C1C=CC(=O)NO)C=CC(=O)C2=CC(=CC=C2)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 激酶实验 [1]: | |
|
玉米HD2, HD1-B,和 HD1-A酶抑制 |
酶使氚化乙酸从底物中释放，使用闪烁计数器定量。IC50值取自三次平行测定结果。将50 μL玉米酶样品（在30 °C下）与10 μL总[3H]醋酸盐标记的鸡网状细胞组蛋白 (2 mg/mL) 一起孵育30分钟。加入50 μL of 1 M HCl/0.4 M乙酸盐和800 μL乙酸乙酯终止上述反应。离心（10000 g，5分钟）后,将600 μL上清液加入到3 mL液体闪烁鸡尾酒中，测定其放射性。MC1568的初始浓度40 μM，再被逐步稀释。以NaB、VPA、TSA、SAHA、85TPX、HC-toxin和tubacin为参考物，空白溶剂作为阴性对照。 |
| 细胞实验 [2]: | |
|
细胞系 |
3T3-L1细胞 |
|
制备方法 |
在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
|
反应条件 |
~ 10 μM；8天 |
|
实验结果 |
在3T3-L1细胞中，MC1568减少PPARγ诱导的脂肪生成 |
| 动物实验 [2]: | |
|
动物模型 |
PPRE-Luc转基因C57BL/6小鼠 |
|
给药剂量 |
50 mg/kg；口服给药；每日1次，持续7天 |
|
实验结果 |
在PPRE-Luc转基因C57BL/6小鼠中，MC1568 (50 mg/kg) 主要损害心脏和脂肪组织的PPARγ信号。 |
|
其它注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同，但仍处于实验系统误差的允许范围内。 |
|
References: [1]. Mai A, Massa S, Pezzi R, Simeoni S, Rotili D, Nebbioso A, Scognamiglio A, Altucci L, Loidl P, Brosch G. Class II (IIa)-selective histone deacetylase inhibitors. 1. Synthesis and biological evaluation of novel (aryloxopropenyl)pyrrolyl hydroxyamides. J Med Chem. 2005 May 5;48(9):3344-53. [2]. Nebbioso A, Dell'Aversana C, Bugge A, Sarno R, Valente S, Rotili D, Manzo F, Teti D, Mandrup S, Ciana P, Maggi A, Mai A, Gronemeyer H, Altucci L. HDACs class II-selective inhibition alters nuclear receptor-dependent differentiation. J Mol Endocrinol. 2010 Oct;45(4):219-28. |
|
| 描述 | MC1568是一种选择性的HDAC抑制剂，作用于玉米HD1-A，IC50值为100 nM，对HD1-A的选择性比HD1-B高34倍。 | |||||
| 靶点 | HD1-A (Maize) | HD1-B (Maize) | ||||
| IC50 | 100 nM | 3400 nM | ||||
质量控制和MSDS
- 批次:
化学结构
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