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CAS No.: 2196203-96-8

TH34 Catalog No. CSN22927

Synonyms: TH34

TH34 is a potent HDAC6/8/10 inhibitor that induces DNA damage-mediated cell death in human high-grade neuroblastoma cell lines.

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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... more >>ght Gain Pregnancy Collapse <<	Not Applicable	Active, not recruiting	September 2018	Germany ... more >> 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 Collapse <<

参考文献

[1] Kolbinger FR, Koeneke E, Ridinger J, Heimburg T, Müller M, Bayer T, Sippl W, Jung M, Gunkel N, Miller AK, Westermann F, Witt O, Oehme I. The HDAC6/8/10 inhibitor TH34 induces DNA damage-mediated cell death in human high-grade neuroblastoma cell lines. Arch Toxicol. 2018 Aug;92(8):2649-2664. doi: 10.1007/s00204-018-2234-8. Epub 2018 Jun 9. PMID: 29947893; PMCID: PMC6063332.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.9017 mL
- 19.5084 mL
- 39.0168 mL
- 5 mM
- 0.7803 mL
- 3.9017 mL
- 7.8034 mL
- 10 mM
- 0.3902 mL
- 1.9508 mL
- 3.9017 mL

技术信息

CAS号

2196203-96-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H16N2O2

运输

蓝冰

分子量

256.30

别名

TH34

溶解度

DMSO	370.0 mg/mL (1443.6 mM)
Water	insoluble

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TH34 Catalog No. CSN22927

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