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    MC1568
    MC1568

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0288
    CAS #: 852475-26-4Purity ≥98%

    Description: MC1568 is a hydroxyamide-based inhibitor of class II histone deacetylase (HDAC) such as HDAC4/5/6/7/9 (IIa) and HDAC6/10 (IIb) with potential antiviral activity. It inhibits influenza A virus replication.

    References: J Med Chem. 2005;48(9):3344-53; J Mol Endocrinol. 2010;45(4):219-28; Diabetes. 2011;60(11):2861-71.

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    Molecular Weight (MW)314.31
    FormulaC17H15FN2O3
    CAS No.852475-26-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 13 mg/mL (41.4 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo) 0.5% CMC: 5 mg/mL
    Synonyms

    MC1568; MC 1568; MC-1568

    Chemical Name: (E)-3-(5-((E)-3-(3-fluorophenyl)-3-oxoprop-1-en-1-yl)-1-methyl-1H-pyrrol-2-yl)-N-hydroxyacrylamide

    InChi Key: QQDIFLSJMFDTCQ-FIFLTTCUSA-N

    InChi Code: InChI=1S/C17H15FN2O3/c1-20-14(5-6-15(20)8-10-17(22)19-23)7-9-16(21)12-3-2-4-13(18)11-12/h2-11,23H,1H3,(H,19,22)/b9-7+,10-8+

    SMILES Code: O=C(NO)/C=C/C1=CC=C(/C=C/C(C2=CC=CC(F)=C2)=O)N1C


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    In Vitro

    In vitro activity: MC1568 is a selective class II (IIa) histone deacetylas (HDAC II) inhibitor with IC50 of 220 nM and 176-fold class II selectivity (against class I). In human breast cancer ZR-75.1 cell lysates, MC1568 (5 μM) shows no inhibitory activity against HDAC1 but is able to inhibit HDAC4. In MCF-7 cells, MC1568 (20 μM) increases the accumulation of acetylated H3 and H4 histones, as well as the levels of acetyl-tubulin, which indicates a inhibitory effect of MC1568 on HDAC6. In C2C12 cells, MC1568 (5 μM) arrests myogenesis by decreasing myocyte enhancer factor 2D (MEF2D) expression, stabilizing the HDAC4-HDAC3-MEF2D complex, and by inhibiting differentiation-induced MEF2D acetylation. MC1568 (5 or 10 μM) interferes with the RAR- and PPARγ-mediated differentiation-inducing signaling pathways. In F9 cells, MC1568 specifically blocks endodermal differentiation despite not affecting retinoic acid-induced maturation of promyelocytic NB4 cells. In 3T3-L1 cells, MC1568 attenuates PPARγ-induced adipogenesis.


    Kinase Assay: The enzyme liberats tritiated acetic acid from the substrate, which is quantified by scintillation counting. IC50 values are results of triple determinations. A 50 μL sample of maize enzyme (at 30 °C) is incubated (30 min) with 10 μL of total [3H]acetate-prelabeled chicken reticulocyte histones (2 mg/mL). Reaction is stopped by addition of 50 μL of 1 M HCl/0.4 M acetate and 800 μL of ethyl acetate. After centrifugation (1×104 g, 5 min), an aliquot of 600 μL of the upper phase is counted for radioactivity in 3 mL of liquid scintillation cocktail. MC1568 is tested at a starting concentration of 40 μM, and active substances are diluted further. NaB, VPA, TSA, SAHA, 85 TPX, HC-toxin, and tubacin are used as the reference compounds, and blank solvents are used as negative controls.


    Cell Assay: The 3T3-L1 cells are propagated and differentiated using a cocktail of isobutylmethylxanthine, dexamethasone, and insulin. From the second day post-confluence and throughout the differentiation period of 8 days, the 3T3-L1 cells are induced by: (1) no induction: at post-confluence and throughout the differentiation period of 8 days, the cells are incubated with DMSO or MC1568. (2) troglitazone: at post-confluence and throughout the differentiation period of 8 days, the cells are induced with 5 μM troglitazone, MC1568, or both. (3) rosiglitazone: at post-confluence and throughout the differentiation period of 8 days, the cells are incubated with 1 μM rosiglitazone and either DMSO or MC1568. (4) rosiglitazone and dexamethasone: at post-confluence, the cells received 1 μM of rosiglitazone and 390 ng/mL dexamethasone. Throughout the differentiation period of 8 days, the cells are induced with 1 μM of rosiglitazone and either DMSO or MC1568. All medium is renewed every second day.

    In VivoIn mice, MC1568 (50 mg/kg) shows an apparent tissue-selective HDAC inhibition. In skeletal muscle and heart, MC1568 inhibits the activity of HDAC4 and HDAC5 without affecting HDAC3 activity, thereby leaving MEF2-HDAC complexes in a repressed state. In reporting PPRE-Luc mice, MC1568 (50 mg/kg) impairs PPARγ signaling mostly in the heart and adipose tissues. In a recent study of pancreatic explants, MC1568 enhances expression of Pax4, a key factor required for proper β-and δ-cell differentiation and amplifies endocrine β- and δ-cells.
    Animal modelPPRE-Luc transgenic mouse (C57BL/6)
    Formulation & DosageDissolved in water solution of 0.5% carbossimetilcellulose; 50 mg/kg; Oral gavage
    References

    J Med Chem. 2005 May 5;48(9):3344-53; J Mol Endocrinol. 2010 Oct;45(4):219-28; Diabetes. 2011 Nov;60(11):2861-71.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    MC1568

     

    MC1568



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