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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C17H15FN2O3 |
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分子量 | 314.31 | CAS No. | 852475-26-4 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 22 mg/mL (69.99 mM) | ||||||||
Water | Insoluble | ||||||||||
Ethanol | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * 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. |
製品説明 | 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 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] |
キナーゼアッセイ | Maize HD2, HD1-B, and HD1-A Enzyme Inhibition. | |
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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. | ||
細胞アッセイ | 細胞株 | 3T3-L1 cells |
濃度 | ~10 μM, dissolved in DMSO | |
反応時間 | 8 days | |
実験の流れ | 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. | |
動物実験 | 動物モデル | PPRE-Luc transgenic mouse (C57BL/6) |
投薬量 | 50 mg/kg | |
投与方法 | By gavage once a day |
Data from [Proc Natl Acad Sci U S A, 2012, 109(34)]
Data from [Proc Natl Acad Sci U S A, 2012, 109(34)]
Data from [PLoS One, 2012, 7(12), e52095]
Selective Inhibition of Histone Deacetylase Class IIa With MC1568 Ameliorates Podocyte Injury [ Front Med (Lausanne), 2022, 9:848938] | PubMed: 35492337 |
HBV covalently closed circular DNA minichromosomes in distinct epigenetic transcriptional states differ in their vulnerability to damage [ Hepatology, 2021, 10.1002/hep.32245] | PubMed: 34779008 |
HBV covalently closed circular DNA minichromosomes in distinct epigenetic transcriptional states differ in their vulnerability to damage [ Hepatology, 2021, 10.1002/hep.32245] | PubMed: 34779008 |
Butyrate and Class I Histone Deacetylase Inhibitors Promote Differentiation of Neonatal Porcine Islet Cells into Beta Cells [ Cells, 2021, 10(11)3249] | PubMed: 34831471 |
Epigenetic Repression of Chloride Channel Accessory 2 Transcription in Cardiac Fibroblast: Implication in Cardiac Fibrosis [ Front Cell Dev Biol, 2021, 9:771466] | PubMed: 34869368 |
HDAC8 cooperates with SMAD3/4 complex to suppress SIRT7 and promote cell survival and migration. [ Nucleic Acids Res, 2020, 6;48(6):2912-2923] | PubMed: 31970414 |
Valproate reverses mania-like behaviors in mice via preferential targeting of HDAC2 [ Mol Psychiatry, 2020, 10.1038/s41380-020-00958-2] | PubMed: 33235333 |
Valproic acid upregulates the expression of the p75NTR/sortilin receptor complex to induce neuronal apoptosis [ Apoptosis, 2020, 10.1007/s10495-020-01626-0] | PubMed: 32712736 |
ΔNp63α promotes the expression and nuclear translocation of PTEN, leading to cisplatin resistance in oral cancer cells [ Am J Transl Res, 2020, 12(10):6187-6203] | PubMed: 33194023 |
Histone Deacetylase Inhibitors Impair Vasculogenic Mimicry from Glioblastoma Cells. [ Cancers (Basel), 2019, 11(6)] | PubMed: 31146471 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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