| 名称 | MC1568 |
| 描述 | 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. |
| 细胞实验 | 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) |
| 激酶实验 | 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. |
| 体外活性 | 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. |
| 体内活性 | 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. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 11 mg/mL (35 mM)
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| 关键字 | HDAC | Histone deacetylases | inhibit | MC-1568 | Inhibitor | MC1568 | MC 1568 |
| 相关产品 | Valproic acid sodium salt | Panobinostat | Theophylline monohydrate | Sodium 4-phenylbutyrate | Vorinostat | Acefylline | Curcumin | Valproic Acid | Parthenolide | 4-Phenylbutyric acid | Theophylline | Methyl L-histidinate dihydrochloride |
| 相关库 | 组蛋白修饰化合物库 | 经典已知活性库 | 表观遗传库 | HIF-1化合物库 | 抑制剂库 | NO PAINS 化合物库 | 抗衰老化合物库 | 已知活性化合物库 | 含氟化合物库 | 抗癌化合物库 |
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