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MC1568 Sale

(Synonyms: MC 1568, MC-1568) 目录号 : GC15965

A selective class IIa HDAC inhibitor

MC1568 Chemical Structure

Cas No.:852475-26-4

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥389.00
现货
10mg
¥368.00
现货
25mg
¥693.00
现货
500mg
¥8,295.00
现货
1g
¥14,553.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Kinase experiment [1]:

Maize HD2, HD1-B, and HD1-A enzyme inhibition

The enzyme liberated tritiated acetic acid from the substrate, which was quantified by scintillation counting. IC50 values are results of triple determinations. A 50 μL sample of maize enzyme (at 30 °C) was incubated (30 mins) with 10 μL of total [3H]acetate-prelabeled chicken reticulocyte histones (2 mg/mL). Reaction was stopped by addition of 50 μL of 1 M HCl/0.4 M acetate and 800 μL of ethyl acetate. After centrifugation (10000 g, 5 mins), an aliquot of 600 μL of the upper phase was counted for radioactivity in 3 mL of liquid scintillation cocktail. MC1568 was tested at a starting concentration of 40 μM, and active substances were diluted further. NaB, VPA, TSA, SAHA, 85TPX, HC-toxin, and tubacin were used as the reference compounds, and blank solvents were used as negative controls.

Cell experiment [2]:

Cell lines

3T3-L1 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months.

Reaction Conditions

~ 10 μM; 8 days

Applications

In 3T3-L1 cells, MC1568 attenuated PPARγ-induced adipogenesis.

Animal experiment [2]:

Animal models

PPRE-Luc transgenic C57BL/6 mice

Dosage form

50 mg/kg; p.o.; q.d., for 7 days

Applications

In PPRE-Luc transgenic C57BL/6 mice, MC1568 (50 mg/kg) impaired PPARγ signaling mostly in the heart and adipose tissues.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

产品描述

MC1568, a derivative of (Aryloxopropenyl)pyrrolyl hydroxyamide, is a novel, potent and specific inhibitor of class II histone deacetylase (HDAC), including two subclasses IIa (HDAC4, HDAC5, HDAC6, HDAC7 and HDAC9) and IIb (HDAC6 and HDAC 10), that exhibits strong inhibition against maize class II HDAC with 50% inhibition concentration IC50 value of 22 μM. MC1568 has been found to tissue-selectively inhibits HDAC and arrest myogenesis in cultured muscle cells through three possible mechanisms, including decreasing the expression of myocyte enhancer factor 2D, stabilizing the HDAC-HDAC3-MEF2D complex and inhibiting the acetylation of differentiation-induced MEF2D. Moreover, MC1568 is able to interfere with RAR- and PPARγ-mediated differentiation-inducing signaling pathways.

Reference

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.

Chemical Properties

Cas No. 852475-26-4 SDF
别名 MC 1568, MC-1568
化学名 (E)-3-[4-[(E)-3-(3-fluorophenyl)-3-oxoprop-1-enyl]-1-methylpyrrol-2-yl]-N-hydroxyprop-2-enamide
Canonical SMILES CN1C=C(C=C1C=CC(=O)NO)C=CC(=O)C2=CC(=CC=C2)F
分子式 C17H15FN2O3 分子量 314.31
溶解度 ≥ 15.7 mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 3.1816 mL 15.9079 mL 31.8157 mL
5 mM 0.6363 mL 3.1816 mL 6.3631 mL
10 mM 0.3182 mL 1.5908 mL 3.1816 mL
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Research Update

1. Class II-specific histone deacetylase inhibitors MC1568 and MC1575 suppress IL-8 expression in human melanoma cells. Pigment Cell Melanoma Res. 2013 Mar;26(2):193-204. doi: 10.1111/pcmr.12049. Epub 2013 Jan 7.
Abstract
MC1568, an HDACi, inhibited IL-8 levels and cell proliferation in unstimulated or PMA-stimulated GR-M and OCM-3 melanoma cell lines through suppressing c-Jun binding to the IL-8 promoter, recruitment of histones 3&4, Rna polymerase II and TFIIB to the IL-8 promoter and c-Jun expression.
2. Improved Synthesis and Structural Reassignment of MC1568: A Class IIa Selective HDAC Inhibitor. J Med Chem. 2014 Feb 13;57(3):1132-5. doi: 10.1021/jm401945k. Epub 2014 Jan 30.
Abstract
MC1568, an inhibitor of class IIa HDAC has been described in terms of synthesis and structural reassignment.