MC1568

Catalog No.S1484

MC1568 Chemical Structure

Molecular Weight(MW): 314.31

MC1568 is a selective HDAC inhibitor for maize HD1-A with IC50 of 100 nM in a cell-free assay. It is 34-fold more selective for HD1-A than HD1-B.

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In DMSO USD 160 In stock
USD 120 In stock
USD 270 In stock
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5 Customer Reviews

  •  

    HDAC4 and OA1 expression correlate inversely during starvation, and HDAC4 inhibition or knockdown leads to OA1 transgene up-regulation. Quantification of OA1 mRNA expression by real-time PCR in HeLa-OA1myc cells at the indicated times of incubation with MC1568 (class II HDACi). Data are expressed as the fold change compared with the amount of the OA1 mRNA in mock conditions at each time point.

    Proc Natl Acad Sci U S A 2012 109(34). MC1568 purchased from Selleck.

     

    HDAC4 is down-regulated during starvation, and its inhibition leads to HIV-1 reactivation in ACH-2 cells. (B) Real-time PCR quantification of US HIV-1 RNA in ACH-2 cells incubated with DMSO (mock of MC1568), MC1568, or TSA at the reported times…(D) 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay for cell viability and proliferation of daily collected supernatants from ACH-2 cells incubated for 3 d.

    Proc Natl Acad Sci U S A 2012 109(34). MC1568 purchased from Selleck.

  • Class-specific histone deacetylase inhibition ameliorates cholesterol accumulation. Mutant fibroblasts (NPC-26) were incubated for 18 h in the presence of the HDAC class-specific inhibitors MC1568 and MGCD0103 (5 μM) and assessed for cholesterol accumulation by filipin fluorescence. Quantification of filipin fluorescence is expressed as arbitrary units. *, p<0.05, treated versus untreated cells by two-tailed Student,s t test.

    J Biol Chem 2011 286, 23842–23851. MC1568 purchased from Selleck.

     

    HDACI sensitivities in pancreatic cancer cell lines and the HPDE cells. Panels A–C: PANC-1 cells were harvested and lysed after incubation with a range of concentrations of MGCD0103 (0–1.0 uM), MC1568 (0–10 uM), or Tubastatin A (0–4 uM) for 96 h. Soluble proteins were analyzed on Western blots probed by anti-acetylated (ac)-H4, -H4, -ac-tubulin, or –b-actin antibody. Panel D: AsPC-1, BxPC-3, PANC-1, or the HPDE cells were cultured at 37’C for 96 h in complete medium in 96-well plates, with a range of concentrations of MGCD0103, MC1568, or Tubastatin A, and cell viabilities were determined using the MTT reagent.

    PLoS One 2012 7(12), e52095. MC1568 purchased from Selleck.

  • Western blot analysis of p-histone and histone. 0-10μM MC1588 was added.

     

     

    2011 Dr. Zhang of Tianjin Medical University. MC1568 purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description MC1568 is a selective HDAC inhibitor for maize HD1-A with IC50 of 100 nM in a cell-free assay. It is 34-fold more selective for HD1-A than HD1-B.
Targets
HD1-A (Maize) [1]
(Cell-free assay)
HD1-B (Maize) [1]
(Cell-free assay)
100 nM 3.4 μM
In vitro

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. [1] 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. [2] 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. [3] 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. [4]

In vivo In 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. [3] In reporting PPRE-Luc mice, MC1568 (50 mg/kg) impairs PPARγ signaling mostly in the heart and adipose tissues. [4] 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. [5]

Protocol

Kinase Assay:[1]
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Maize HD2, HD1-B, and HD1-A Enzyme Inhibition.:

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 Research:[4]
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  • Cell lines: 3T3-L1 cells
  • Concentrations: ~10 μM, dissolved in DMSO
  • Incubation Time: 8 days
  • Method: 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.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: PPRE-Luc transgenic mouse (C57BL/6)
  • Formulation: Dissolved in water solution of 0.5% carbossimetilcellulose
  • Dosages: 50 mg/kg
  • Administration: By gavage once a day
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 13 mg/mL (41.36 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
0.5% CMC
5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 314.31
Formula

C17H15FN2O3

CAS No. 852475-26-4
Storage powder
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID