| 名稱 | 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. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 在胰臟移植研究中,MC1568增強(qiáng)內(nèi)分泌β和δ-cells細(xì)胞,并使Pax4的表達(dá)增強(qiáng). 在鼠體內(nèi),MC1568（50 mg/kg）組織選擇性地顯著抑制HDAC. 在PPRE-Luc鼠體內(nèi),MC1568（50 mg/kg）主要損害心臟和脂肪組織部位PPARγ信號(hào).作用于骨骼肌和心臟時(shí),MC1568抑制HDAC4/5的活性,不影響HDAC3活性,故MEF2-HDAC復(fù)合體處于未激活狀態(tài). |
| 體內(nèi)活性 | MC1568對(duì)HDAC II的選擇性抑制效果（IC50：220 nM）是I型的176倍。作用于C2C12細(xì)胞時(shí),MC1568（5 μM）通過(guò)降低肌細(xì)胞增強(qiáng)因子2D的表達(dá),使HDAC4-HDAC3-MEF2D復(fù)合體穩(wěn)定,并抑制分化誘導(dǎo)的MEF2D乙?；?從而使肌細(xì)胞生成被阻斷。MC1568（5或10 μM）可使RAR和PPARγ調(diào)節(jié)的分化誘導(dǎo)信號(hào)通路受干擾。 在MCF-7細(xì)胞中,MC1568（20 μM）使乙?；疕3和H4組蛋白的累積增強(qiáng),并提高乙?；⒐艿鞍椎乃?表明MC1568可抑制HDAC6。作用于人類乳腺癌ZR-75.1細(xì)胞裂解物時(shí),MC1568對(duì)HDAC1無(wú)抑制作用,但是可使HDAC4受抑制。作用于F9細(xì)胞時(shí),MC1568選擇性抑制內(nèi)胚分化,對(duì)VA誘導(dǎo)的早幼粒NB4細(xì)胞成熟無(wú)影響。作用于3T3-L1細(xì)胞時(shí),MC1568使PPARγ誘導(dǎo)的脂肪生成降低。 |
| 存儲(chǔ)條件 | 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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| 關(guān)鍵字 | HDAC | Histone deacetylases | inhibit | MC-1568 | Inhibitor | MC1568 | MC 1568 |
| 相關(guān)產(chǎn)品 | Valproic acid sodium salt | 4-Phenylbutyric acid | Valproic Acid | Panobinostat | Methyl L-histidinate dihydrochloride | Theophylline | Acefylline | Curcumin | Theophylline monohydrate | Sodium 4-phenylbutyrate | Vorinostat | Parthenolide |
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