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MC1568

Catalog No. T2023   CAS 852475-26-4

MC1568 is a specific HDAC inhibitor for maize HD1-A (IC50: 100 nM, in a cell-free assay). It is 34-fold more selective for HD1-A than HD1-B.

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MC1568 Chemical Structure
MC1568, CAS 852475-26-4
Pack Size Availability Price/USD Quantity
5 mg In stock $ 32.00
10 mg In stock $ 52.00
25 mg In stock $ 94.00
50 mg In stock $ 145.00
100 mg In stock $ 262.00
200 mg In stock $ 455.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 98.98%
Purity: 98%
Purity: 89.82%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MC1568 is a specific HDAC inhibitor for maize HD1-A (IC50: 100 nM, in a cell-free assay). It is 34-fold more selective for HD1-A than HD1-B.
Targets&IC50 HD1-A (Maize):100 nM
In vitro In pancreatic transplantation research, MC1568 significantly enhances endocrine β and δ-cells and increases the expression of Pax4. In vivo in mice, MC1568 (50 mg/kg) selectively and markedly inhibits HDAC. Within PPRE-Luc mice, MC1568 (50 mg/kg) specifically disrupts PPARγ signaling in the heart and adipose tissues. When acting on skeletal muscle and heart, MC1568 inhibits the activity of HDAC4/5 without affecting HDAC3 activity, leaving the MEF2-HDAC complex in an inactive state.
In vivo MC1568 selectively inhibits HDAC class II with an IC50 of 220 nM, showing 176 times greater selectivity compared to class I HDACs. In C2C12 cells, MC1568 (5 μM) stabilizes the HDAC4-HDAC3-MEF2 (Myocyte Enhancer Factor 2D) complex by reducing MEF2D expression, blocking myogenic differentiation through inhibition of MEF2D acetylation. Additionally, MC1568 at 5 or 10 μM disrupts the RAR (Retinoic Acid Receptor) and PPARγ (Peroxisome Proliferator-Activated Receptor Gamma)-mediated differentiation signaling pathways. In MCF-7 cells, a concentration of 20 μM MC1568 enhances the accumulation of acetylated H3 and H4 histones and acetylated tubulin levels, indicating inhibition of HDAC6. Experiments with human breast cancer ZR-75.1 cell lysates show that MC1568 does not inhibit HDAC1 but does inhibit HDAC4. In F9 cells, MC1568 selectively inhibits endodermal differentiation without affecting VA (Vitamin A)-induced maturation in early promyelocytic NB4 cells. Furthermore, in 3T3-L1 cells, MC1568 reduces PPARγ-induced adipogenesis.
Kinase Assay 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 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)
Molecular Weight 314.31
Formula C17H15FN2O3
CAS No. 852475-26-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 11 mg/mL (35 mM)

TargetMolReferences and Literature

1. Mai A, et al. J Med Chem, 2005, 48(9), 3344-3353. 2. Duong V, et al. Mol Cancer Res, 2008, 6(12), 1908-1919. 3. Nebbioso A, et al. EMBO Rep, 2009, 10(7), 776-782. 4. Nebbioso A, et al. J Mol Endocrinol, 2010, 45(4), 219-228. 5. Lenoir O, et al. Diabetes, 2011, 60(11), 2861-2871. 6. Kassis H, et al. Class IIa histone deacetylases affect neuronal remodeling and functional outcome after stroke. Neurochem Int. 2016 Jun;96:24-31.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library NO PAINS Compound Library Immunology/Inflammation Compound Library Reprogramming Compound Library NF-κB Signaling Compound Library Bioactive Compounds Library Max Epigenetics Compound Library Anti-Breast Cancer Compound Library DNA Damage & Repair Compound Library Covalent Inhibitor Library

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Keywords

MC1568 852475-26-4 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Histone deacetylases inhibit MC-1568 Inhibitor MC 1568 inhibitor

 

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