Vorinostat (SAHA, MK0683)是一种I和II类组蛋白去乙酰化酶(HDAC)抑制剂，IC50小于86 nM。可用于皮肤T细胞淋巴瘤的相关研究。
别名：SAHA; Zolinza; MK-0683; Suberoylanilide hydroxamic acid
Vorinostat (SAHA, MK0683)是一种I和II类组蛋白去乙酰化酶(HDAC)抑制剂，IC50小于86 nM。Vorinostat是小分子量（<300）线性肟酸，抑制HDAC活性，包括乙酰化组蛋白和非组蛋白的积累，抑制培养细胞的增殖，且抑制肿瘤生长。Vorinostat通过结合到酶的活性位点而抑制 HDAC活性。Vorinostat 抑制多种转化细胞增殖（包括 淋巴瘤，多发性骨髓瘤，白血病，和非小细胞肺癌），与对照组相比抑制生长达50% 时的浓度为0.5 到10μM。
BMC Cancer. 2016 Nov 7;16(1):857.
Vorinostat enhances the cisplatin-mediated anticancer effects in small cell lung cancer cells.
 . figure 6..jpg) |
数据来源 | BMC Cancer (2016) . Figure 6. Vorinostat (purity >99 %) was purchased from AbMole BioScience (Houston, TX, USA) |
| 方法 | Antitumor activity in H209 xenografts | |
| 细胞系/动物模型 | H209 cells line | |
| 浓度 | 40mg/kg 4 times a week | |
| 处理时间 | 5 weeks | |
| 实验结果 | As presented in Fig. 6, compared with vehicle and single-agent treatments, the combination treatment significantly inhibited tumor growth at day 5. |
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数据来源 | BMC Cancer (2016) . Figure 5. Vorinostat (purity >99 %) was purchased from AbMole BioScience (Houston, TX, USA) |
| 方法 | western blot | |
| 细胞系/动物模型 | H209 and H146 cells line | |
| 浓度 | 0.05, 0.1 and 0.2 μ M | |
| 处理时间 | 24 h | |
| 实验结果 | As presented in Fig. 5a and b, vorinostat alone induced a dose-dependent reduction of TS protein levels in the H209 and H146 cells. |
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数据来源 | BMC Cancer (2016) . Figure 4. Vorinostat (purity >99 %) was purchased from AbMole BioScience (Houston, TX, USA) |
| 方法 | flow cytometry | |
| 细胞系/动物模型 | H209 and H146 cells line | |
| 浓度 | 0.1 μ M | |
| 处理时间 | 24 h | |
| 实验结果 | The H146 cells treated with vorinostat demonstrated no distinct cell cycle arrest, whereas those treated with cisplatin exhibited cell cycle arrest in the S phase (Fig. 4b and d). Similarly, the combination treatment induced cell cycle arrest in the S phase in the H146 cells. |
 . figure 3..jpg) |
数据来源 | BMC Cancer (2016) . Figure 3. Vorinostat (purity >99 %) was purchased from AbMole BioScience (Houston, TX, USA) |
| 方法 | caspase-3 activity assay and Western blot | |
| 细胞系/动物模型 | H209 and H146 cells line | |
| 浓度 | 0, 0.05, 0.1 and 0.2 μ M | |
| 处理时间 | 24 or 36 h | |
| 实验结果 | Therefore, our data indicated that the combination treatment dose dependently increased apoptosis in the proteolytic cleavage of PARP and activated caspase-3 in SCLC cells. |
 . figure 2..jpg) |
数据来源 | BMC Cancer (2016) . Figure 2. Vorinostat (purity >99 %) was purchased from AbMole BioScience (Houston, TX, USA) |
| 方法 | Cell viability assay and Western blot | |
| 细胞系/动物模型 | H209 and H146 cells line | |
| 浓度 | 0, 0.1 or 0.2 μ M | |
| 处理时间 | 24 h | |
| 实验结果 | The combination treatments were more effective in inhibiting H209 cell viability in a dosedependent manner (Fig. 2a). Specifically, the cell viabilities observed when the cells were treated with combinations of cisplatin at 5 μM and vorinostat at 0.1 or 0.2 μM were 80.21 and 68.81 %, respectively (Fig. 2b). |
 . figure 1..jpg) |
数据来源 | BMC Cancer (2016) . Figure 1. Vorinostat (purity >99 %) was purchased from AbMole BioScience (Houston, TX, USA) |
| 方法 | Cell viability assay and Western blot | |
| 细胞系/动物模型 | H209 and H146 cells line | |
| 浓度 | 0, 0.4 or 0.8 μ M | |
| 处理时间 | 24 h | |
| 实验结果 | Overall, these results indicated that the triple combination treatment enhanced cytotoxic effects and promoted apoptosis in SCLC cells. |
| 体外实验* | |
|---|---|
| 细胞系 | HH, HuT78, MJ, MylA and SeAx cells |
| 方法 | cell viability assay. The inhibitory effect of vorinostat on the viability of CTCL cell lines was examined through a CellTiter-Glo assay using various concentrations of vorinostat (0.01, 0.05, 0.15, 0.5, 1.25, 4, 10, 35, and 100 μM) for 72 h. All CTCL cell lines were sensitive to the investigated HDAC inhibitor. The inhibitory effect of vorinostat was reflected as a dose-dependent reduction in cell proliferation/viability. The IC50 of proliferation was determined at 0.146 μM in HH cells, at 2.062 μM in HuT78 cells, at 2.697 μM in MJ cells, at 1.375 μM in MylA and at 1.510 μM in SeAx cells. |
| 浓度 | 0.01, 0.05, 0.15, 0.5, 1.25, 4, 10, 35, and 100 μM |
| 处理时间 | 72 h |
*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。
| 体内实验* | |
|---|---|
| 动物模型 | R6/2 mice motor impair |
| 配制 | solubilized in 5 molar equivalents of HOP-β-CD (ICN) in water |
| 剂量 | 0.67g/L |
| 给药处理 | orally |
*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。
| 分子量 | 264.3 |
| 分子式 | C14H20N2O3 |
| CAS号 | 149647-78-9 |
| 溶解性（25°C） | DMSO 55 mg/mL |
| 储存条件 |
粉末型式 -20°C 3年；4°C 2年 溶于溶剂 -80°C 6个月；-20°C 1个月 |
| 运输方式 | 冰袋运输，根据产品的不同，可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.7836 mL | 18.9179 mL | 37.8358 mL |
| 5 mM | 0.7567 mL | 3.7836 mL | 7.5672 mL |
| 10 mM | 0.3784 mL | 1.8918 mL | 3.7836 mL |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
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|---|
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Ac-Arg-Gly-Lys(Ac)-AMC 是 HDAC 的一个底物。 |
| Chlamydocin
Chlamydocin，一种真菌代谢产物，是一种高效的 HDAC 抑制剂，IC50 为 1.3 nM。 |
| HDAC-IN-30
HDAC-IN-30 是一种新颖的多靶点 HDAC 抑制剂，靶点主要有 HDAC1 (IC50=13.4 nM)，HDAC2 (IC50=28.0 nM)， HDAC3 (IC50=9.18 nM)，HDAC6 (IC50=42.7 nM)，HDAC8 (IC50=131 nM)。 |
| Ac-Arg-Gly-Lys(Ac)-AMC acetate
Ac-Arg-Gly-Lys(Ac)-AMC acetate是组蛋白去乙酰酶（HDAC）的一个底物，可用于HDAC活性的新型荧光检测。 |
| JPS014 TFA
JPS014 TFA 是一种基于苯甲酰胺的 Von Hippel-Lindau (VHL) E3-连接酶蛋白水解靶向嵌合体 (PROTAC)。 |
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