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MC1568

MC1568 is a selective HDAC inhibitor with IC50 of 220 nM.

Catalog No.S1484

5 Reviews 6 Product Citations

: Tel: +1-832-582-8158[email protected]

MC1568 Chemical Structure
Molecular Weight: 314.31

Validation & Quality Control

Product Citations(6)

Proc Natl Acad Sci U S A, 2012, 109(34):E2284-93

J Biol Chem, 2011, 286(27), 23842-23851

J Biol Chem, 2011, 286(18), 16101-16108

Mol Pharm, 2013, 10(1):307-18

J Biol Chem, 2011, 286(18):16101-8
PLoS One, 2012, 7(12):e52095

Customer Reviews(5) in vivo invitation

Related Compound Libraries

MC1568 is available in the following compound libraries:

Chemical Library (96-well) Epigenetics Compound Library (96-well) Inhibitor Library (96-well)

Product Information

Compare HDAC Inhibitors

Research Area
Research Area
Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S1053	Entinostat (MS-275, SNDX-275)	<1 mg/mL	75 mg/mL	<1 mg/mL
S1047	Vorinostat (SAHA)	<1 mg/mL	53 mg/mL	3 mg/mL
S1030	Panobinostat (LBH589)	<1 mg/mL	70 mg/mL	<1 mg/mL
S3020	Romidepsin (FK228 ,depsipeptide)	<1 mg/mL	10 mg/mL	<1 mg/mL
S1045	Trichostatin A (TSA)	<1 mg/mL	23 mg/mL	<1 mg/mL
S1122	Mocetinostat (MGCD0103)	<1 mg/mL	13 mg/mL	<1 mg/mL
S2627	Tubastatin A HCl	<1 mg/mL	74 mg/mL	<1 mg/mL
S1085	Belinostat (PXD101)	<1 mg/mL	64 mg/mL	<1 mg/mL
S2170	ITF2357 (Givinostat)	<1 mg/mL	95 mg/mL	3 mg/mL
S1095	LAQ824 (NVP-LAQ824, Dacinostat)	<1 mg/mL	76 mg/mL	<1 mg/mL
S1194	CUDC-101	<1 mg/mL	20 mg/mL	<1 mg/mL
S1515	SB939 (Pracinostat)	<1 mg/mL	72 mg/mL	27 mg/mL
S2012	PCI-34051	<1 mg/mL	59 mg/mL	<1 mg/mL
S1422	Droxinostat	<1 mg/mL	49 mg/mL	49 mg/mL
S1484	MC1568	<1 mg/mL	13 mg/mL	<1 mg/mL
S1090	PCI-24781	<1 mg/mL	80 mg/mL	<1 mg/mL
S1096	JNJ-26481585	<1 mg/mL	79 mg/mL	<1 mg/mL
S1168	Valproic acid sodium salt (Sodium valproate)	33 mg/mL	33 mg/mL	33 mg/mL
S2818	CI994 (Tacedinaline)	<1 mg/mL	≥54 mg/mL	<1 mg/mL
S2244	AR-42 (HDAC-42)	<1 mg/mL	63 mg/mL	63 mg/mL
S2779	M344	<1 mg/mL	62 mg/mL	4 mg/mL
S2759	PI3K/HDAC InhibitorⅠ	<1 mg/mL	102 mg/mL	<1 mg/mL
S8001	Rocilinostat (ACY-1215)	<1 mg/mL	87 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Chemical Information Customer Reviews Product Citations Tech Support & FAQs

Biological Activity

Description	MC1568 is a selective HDAC inhibitor with IC50 of 220 nM.
Targets	HDAC
IC50	220 nM ^[1]
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]
Clinical Trials
Features

Protocol(Only for Reference)

Kinase Assay: ^[1]

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.

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 Assay: ^[4]

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.

Animal Study: ^[4]

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

References

Chemical Information

Download MC1568 SDF

Molecular Weight (MW)	314.31
Formula	C₁₇H₁₅FN₂O₃
CAS No.	852475-26-4, 1003600-29-0
Synonyms	N/A

Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name	(E)-3-(4-((E)-3-(3-fluorophenyl)-3-oxoprop-1-enyl)-1-methyl-1H-pyrrol-2-yl)-N-hydroxyacrylamide

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Research Area

Customer Reviews (5)

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Rating

Source

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

Method

Real time PCR

Cell Lines

HeLa-OA1myc cells

Concentrations

20 uM

Incubation Time

30-120 h

Results

To investigate the functional role of HDAC4 in transgene derepression, we incubated HeLa-OA1myc cells with MC1568, a selective inhibitor of class II HDAC enzymatic activity . The treatment led to an increase of about twofold in the OA1 mRNA at every examined time point (Fig. C).

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Rating

Source

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

Method

Real time PCR

Cell Lines

ACH-2 cells

Concentrations

5-10 uM

Incubation Time

6-72 h

Results

ACH-2 cells were incubated with the selective class II HDACi MC1568, and this resulted in a significant increase of HIV-1 mRNA at all tested time points, with a peak of 60-fold after 24 h of incubation (Fig. 5B)…Overall, TSA showed a more potent effect than MC1568 in terms of induction of both HIV-1 mRNA transcription and RT activity production (Fig. 5 B and C); however, it also caused an earlier and more dramatic loss of cell viability (Fig. 5D).

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Rating

Source

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

Method

Western blot

Cell Lines

PANC1/AsPc-1/BxPC-3/HPDE cells

Concentrations

1.25-10 uM

Incubation Time

96 h

Results

Treatments of PANC-1 cells with variable concentrations of MGCD0103 (0–1.0 uM) resulted in a dose-dependent hyperacetylation of histone H4, while having no effects on alpha-tubulin (a HDAC6 substrate) acetylation or total H4 levels (Figure 2A). Treatments with MC1568 also resulted in acetylation of histone H4 (obvious at 5 and 10 uM), however, to a much lesser extent compared to MGCD0103, and the levels of acetylated histone H4 plateaued at 5 and 10 uM. Further, these treatments had no impact on alpha-tubulin acetylation.

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Rating

Source

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

Method

Western blotting

Cell Lines

Concentrations

0-10 µM

Incubation Time

Results

Increased Histone H3 acetylation with MC1568 treatment was observed.

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Rating

Source

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

Method

Filipin fluorescence

Cell Lines

NPC-26 cells

Concentrations

5 µM

Incubation Time

18 h

Results

The HDAC class-specific inhibitors MC1568 and MGCD0103 (5 µM) also reduced filipin accumulation in NPC-26 compared with untreated cells after 24 h of treatment.

Product Citations (6)

Amino acid starvation induces reactivation of silenced transgenes and latent HIV-1 provirus via down-regulation of histone deacetylase 4 (HDAC4). [Palmisano I, et al. Proc Natl Acad Sci U S A 2012;109(34):E2284-93]
PubMed: 22826225
An "Exacerbate-reverse" strategy in yeast identifies histone deacetylase inhibition as a correction for cholesterol and sphingolipid transport defects in human Niemann-Pick type C disease. [Munkacsi AB, et al. J Biol Chem 2011;286(27), 23842-23851]
PubMed: 21489983
Suberoylanilide hydroxamic acid (Vorinostat) up-regulates progranulin transcription: rational therapeutic approach to frontotemporal dementia. [Cenik B, et al. J Biol Chem 2011;286(18), 16101-16108]
PubMed: 21454553

Inhibition of Multiple Pathogenic Pathways by Histone Deacetylase Inhibitor SAHA in a Corneal Alkali-Burn Injury Model. [Li X, et al. Mol Pharm 2013;10(1):307-18]
PubMed: 23186311
SAHA (VORINOSTAT) upregulates progranulin transcription: a rational therapeutic approach to frontotemporal dementia. [Cenik B, et al. J Biol Chem 2011;286(18):16101-8]
PubMed: 21454553
Class I and Class II Histone Deacetylases Are Potential Therapeutic Targets for Treating Pancreatic Cancer. [Wang G, et al. PLoS One 2012;7(12):e52095]
PubMed: 23251689

Tech Support & FAQs

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3Monday–Friday 9:00 AM–5:00 PM (Central Time)

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Mocetinostat (MGCD0103)

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Product Categories

MC1568

Validation & Quality Control

Product Citations(6)

Customer Reviews(5) in vivo invitation

Related Compound Libraries

MC1568 is available in the following compound libraries:

Product Information

Compare HDAC Inhibitors

Research Area

Product Description

Biological Activity

Protocol(Only for Reference)

Kinase Assay: ^[1]

Cell Assay: ^[4]

Animal Study: ^[4]

References

Chemical Information

Research Area

Customer Reviews (5)

Product Citations (6)

Tech Support & FAQs

If you have any other enquiries, please leave a message.

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S1030	Panobinostat (LBH589)	<1 mg/mL	70 mg/mL	<1 mg/mL
S3020	Romidepsin (FK228 ,depsipeptide)	<1 mg/mL	10 mg/mL	<1 mg/mL
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S2627	Tubastatin A HCl	<1 mg/mL	74 mg/mL	<1 mg/mL
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S2818	CI994 (Tacedinaline)	<1 mg/mL	≥54 mg/mL	<1 mg/mL
S2244	AR-42 (HDAC-42)	<1 mg/mL	63 mg/mL	63 mg/mL
S2779	M344	<1 mg/mL	62 mg/mL	4 mg/mL
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S8001	Rocilinostat (ACY-1215)	<1 mg/mL	87 mg/mL	<1 mg/mL

Choose Your Country or Region

Product Categories

MC1568

Validation & Quality Control

Product Citations(6)

Customer Reviews(5) in vivo invitation

Related Compound Libraries

MC1568 is available in the following compound libraries:

Product Information

Compare HDAC Inhibitors

Research Area

Product Description

Biological Activity

Protocol(Only for Reference)

Kinase Assay: [1]

Cell Assay: [4]

Animal Study: [4]

References

Chemical Information

Research Area

Customer Reviews (5)

Product Citations (6)

Tech Support & FAQs

If you have any other enquiries, please leave a message.

Related HDAC Inhibitors

Recently Viewed Items

E-newsletter

Kinase Assay: ^[1]

Cell Assay: ^[4]

Animal Study: ^[4]