TH34
产品说明书
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同义名 : | - |
| CAS号 : | 2196203-96-8 | |
| 货号 : | A813621 | |
| 分子式 : | C15H16N2O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 256.3 | |
| MDL号 : | MFCD31812450 | |
| 存储条件： |
Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 145 mg/mL(565.74 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The histone deacetylase (HDAC) family consists of 11 subtypes that are responsible for catalyzing the removal of acetyl groups from lysine residues of nuclear and cytoplasmic substrates. TH34 is a potent, small molecule inhibitor of HDAC6/8/10 with IC50 values of 4.6, 1.9, and 7.7 µM, respectively. Treatment of SK-N-BE(2)-C neuroblastoma cells with 25 µM TH34 strongly induced the accumulation of acidic vesicles when compared to non-TH34-treated controls. Incubation with TH34 at 25 µM for 4 days induced caspase-dependent programmed cell death in neuroblastoma cell lines, whereas the effect was moderate in medulloblastoma cells. Treatment with TH34 at 10 and 25 µM for 72 hours significantly increased the subG1 fraction of SK-N-BE(2)-C cells in a dose-dependent manner. When treating proliferating non-malignant fibroblasts (VH7 cells) with TH34 at 25 µM, limited cytotoxic effects were observed in these fibroblasts. After 72h treatment with 10 µM TH34, SK-N-BE(2)-C neuroblastoma cells showed significantly higher expression of neurotrophic receptor tyrosine kinase 1 as compared to non-treated control cells. After 6 days of TH34 treatment (10 and 25 µM), the number and length of neurites were significantly increased in SK-N-BE(2)-C cells. It was also showed that TH34 induced DNA damage in high-grade neuroblastoma cells. Treatment of NB8 and Kelly cells with TH34 resulted in a reduction of cellular metabolic activity with IC50 values of 47.3 and 39.1 µM, respectively[1]. | ||
| 作用机制 | TH34 inhibits HDAC6/8/10 by inducing the hyperacetylation of their substrates (i.e. tubulin and SMC3). | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01958307 | Lifestyle Wei... 展开 >>ght Gain Pregnancy 收起 << | Not Applicable | Active, not recruiting | September 2018 | Germany ... 展开 >> AELF, Fachzentrum L 3.10 Ernährung/Gemeinschaftsverpflegung Bayreuth, Germany, 95447 AELF, Fachzentrum L 3.10 Ernährung/Gemeinschaftsverpflegung Fürstenfeldbruck, Germany, 82256 AELF, Fachzentrum L 3.10 Ernährung/Gemeinschaftsverpflegung Fürth, Germany, 90763 AELF, Fachzentrum L 3.10 Ernährung/Gemeinschaftsverpflegung Regensburg, Germany, 93057 AELF, Fachzentrum L 3.10 Ernährung/Gemeinschaftsverpflegung Würzburg, Germany, 97074 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.90mL 0.78mL 0.39mL |
19.51mL 3.90mL 1.95mL |
39.02mL 7.80mL 3.90mL |
| 参考文献 |
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