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TH34 {[allProObj[0].p_purity_real_show]}

货号:A813621

TH34是一种有效的 HDAC6/8/10 抑制剂,可诱导人高等级神经母细胞瘤细胞系中的 DNA 损伤介导的细胞死亡。

TH34 化学结构 CAS号:2196203-96-8
TH34 化学结构
CAS号:2196203-96-8
TH34 3D分子结构
CAS号:2196203-96-8
TH34 化学结构 CAS号:2196203-96-8
TH34 3D分子结构 CAS号:2196203-96-8
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TH34 纯度/质量文件 产品仅供科研

货号:A813621 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 HD1 HD2 HDAC HDAC1 HDAC10 HDAC11 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 其他靶点 纯度
Givinostat HCl monohydrate ++++

HD1-B, IC50: 7.5 nM

HD1-A, IC50: 16 nM

+++

HD2, IC50: 10 nM

99%+
MC1568 ++

HD1-B (Maize), IC50: 3.4 μM

HD1-A (Maize), IC50: 100 nM

96%
Trichostatin A ++++

HDAC, IC50: ~1.8 nM

99%+
Scriptaid 99%+
Valproic acid sodium Autophagy 97%
AR-42 +++

HDAC, IC50: 30 nM

99%+
Dacinostat +++

HDAC, IC50: 32 nM

98+%
CUDC-101 ++++

HDAC, IC50: 4.4 nM

++++

HDAC1, IC50: 4.5 nM

+++

HDAC10, IC50: 26.1 nM

+++

HDAC2, IC50: 12.6 nM

++++

HDAC3, IC50: 9.1 nM

+++

HDAC4, IC50: 13.2 nM

+++

HDAC5, IC50: 11.4 nM

++++

HDAC6, IC50: 5.1 nM

+

HDAC7, IC50: 373 nM

++

HDAC8, IC50: 79.8 nM

++

HDAC9, IC50: 67.2 nM

EGFR,HER2 99%+
M344 ++

HDAC, IC50: 100 nM

99%+
Splitomicin +

Sir2p, IC50: 60 μM

99%
Panobinostat ++++

HDAC (Reh cells), IC50: 20 nM

HDAC (MOLT-4 cells), IC50: 5 nM

98%
Sodium 4-Phenylbutyrate 98%
Vorinostat +++

HDAC, IC50: ~10 nM

98%
Curcumin NF-κB,Nrf2 98%
Belinostat +++

HDAC, IC50: 27 nM

98%
RG-2833 ++

HDAC1, Ki: 32 nM

++

HDAC3, Ki: 5 nM

98%
Valproic acid +

HDAC1, IC50: 0.4 mM

98%
BG45 +

HDAC1, IC50: 2 μM

+

HDAC2, IC50: 2.2 μM

+

HDAC3, IC50: 289 nM

99%+
Entinostat +

HDAC1, IC50: 0.51 μM

+

HDAC3, IC50: 1.7 μM

98%
Resminostat +++

HDAC1, IC50: 42.5 nM

++

HDAC3, IC50: 50.1 nM

++

HDAC6, IC50: 71.8 nM

98+%
Romidepsin +++

HDAC1, IC50: 36 nM

+++

HDAC2, IC50: 47 nM

99%+
Parthenolide NF-κB,p53 97% HPLC
Tacedinaline +

HDAC1, IC50: 0.9 μM

+

HDAC2, IC50: 0.9 μM

+

HDAC3, IC50: 1.2 μM

98%
Mocetinostat ++

HDAC1, IC50: 0.15 μM

+

HDAC11, IC50: 0.59 μM

+

HDAC2, IC50: 0.29 μM

+

HDAC3, IC50: 1.66 μM

98%
WT-161 ++++

HDAC1, IC50: 8.35 nM

+++

HDAC2, IC50: 15.4 nM

++++

HDAC6, IC50: 0.4 nM

99%+
Fimepinostat ++++

HDAC1, IC50: 1.7 nM

++++

HDAC10, IC50: 2.8 nM

++++

HDAC11, IC50: 5.4 nM

++++

HDAC2, IC50: 5.0 nM

++++

HDAC3, IC50: 1.8 nM

+++

HDAC6, IC50: 27 nM

99%+
Tucidinostat ++

HDAC1, IC50: 95 nM

++

HDAC10, IC50: 78 nM

++

HDAC2, IC50: 160 nM

++

HDAC3, IC50: 67 nM

99%+
Santacruzamate A ++++

HDAC2, IC50: 119 pM

99%+
(E,E)-RGFP966 ++

HDAC3, IC50: 80 nM

99%+
LMK-235 +++

HDAC4, IC50: 11.9 nM

++++

HDAC5, IC50: 4.2 nM

99%+
Tasquinimod 99%+
CAY10603 ++++

HDAC6, IC50: 2 pM

98%
Tubastatin A +++

HDAC6, IC50: 15 nM

98%
Tubacin ++++

HDAC6, IC50: 4 nM

99%+
ACY-738 ++++

HDAC6, IC50: 1.7 nM

99%+
Nexturastat A ++++

HDAC6, IC50: 5 nM

99%+
BRD73954 +++

HDAC6, IC50: 36 nM

++

HDAC8, IC50: 120 nM

99%
Tubastatin A HCl +++

HDAC6, IC50: 15 nM

+

HDAC8, IC50: 854 nM

98%
PCI-34051 +++

HDAC8, IC50: 10 nM

99%+
Ricolinostat ++

HDAC1, IC50: 58 nM

++

HDAC2, IC50: 48 nM

++

HDAC3, IC50: 51 nM

++++

HDAC6, IC50: 4.7 nM

++

HDAC8, IC50: 100 nM

99%+
Droxinostat +

HDAC3, IC50: 16.9 μM

+

HDAC6, IC50: 2.47 μM

+

HDAC8, IC50: 1.46 μM

99%+
Abexinostat ++++

HDAC1, Ki: 7 nM

+++

HDAC10, IC50: 24 nM

+++

HDAC2, Ki: 19 nM

++++

HDAC3/SMRT, Ki: 8.2 nM

+++

HDAC6, Ki: 17 nM

+

HDAC8, IC50: 280 nM

98%+
Citarinostat +++

HDAC1, IC50: 35 nM

+++

HDAC2, IC50: 45 nM

+++

HDAC3, IC50: 46 nM

++++

HDAC6, IC50: 2.6 nM

++

HDAC8, IC50: 137 nM

99%+
HPOB +

HDAC1, IC50: 2.9 μM

+

HDAC10, IC50: 3.0 μM

+

HDAC2, IC50: 4.4 μM

+

HDAC3, IC50: 1.7 μM

++

HDAC6, IC50: 56 nM

+

HDAC8, IC50: 2.8 μM

97%
Quisinostat 2HCl ++++

HDAC1, IC50: 0.11 nM

++++

HDAC10, IC50: 0.46 nM

++++

HDAC11, IC50: 0.37 nM

++++

HDAC2, IC50: 0.33 nM

++++

HDAC3, IC50: 4.86 nM

++++

HDAC4, IC50: 0.64 nM

++++

HDAC5, IC50: 3.69 nM

++++

HDAC8, IC50: 4.26 nM

97%
Domatinostat +

HDAC1, IC50: 1.20 μM

+

HDAC10, IC50: 21 μM

+

HDAC11, IC50: 9.7 μM

+

HDAC2, IC50: 1.12 μM

+

HDAC3, IC50: 0.57 μM

+

HDAC5, IC50: 11.3 μM

+

HDAC9, IC50: 50 μM

99%+
TMP269 ++

HDAC4, IC50: 157 nM

++

HDAC5, IC50: 97 nM

+++

HDAC7, IC50: 43 nM

+++

HDAC9, IC50: 23 nM

99%+
Pracinostat ++

HDAC1, IC50: 49 nM

+++

HDAC10, IC50: 40 nM

++

HDAC11, IC50: 93 nM

++

HDAC2, IC50: 96 nM

+++

HDAC3, IC50: 43 nM

++

HDAC4, IC50: 56 nM

+++

HDAC5, IC50: 47 nM

+

HDAC6, IC50: 1.008 μM

++

HDAC7, IC50: 137 nM

++

HDAC8, IC50: 140 nM

++

HDAC9, IC50: 70 nM

99%+
TMP195 ++

HDAC4, Ki: 59 nM

++

HDAC5, Ki: 60 nM

+++

HDAC7, Ki: 26 nM

+++

HDAC9, Ki: 15 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

TH34 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).

TH34 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 <<

TH34 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.

TH34 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.90mL

0.78mL

0.39mL

19.51mL

3.90mL

1.95mL

39.02mL

7.80mL

3.90mL

TH34 技术信息

CAS号2196203-96-8
分子式C15H16N2O2
分子量 256.3
SMILES Code O=C(NO)C1=CC=C(C)C(NCC2=CC=CC=C2)=C1
MDL No. MFCD31812450
别名
运输蓝冰
InChI Key PZBARTUEWCQNSN-UHFFFAOYSA-N
Pubchem ID 134159676
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, room temperature

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
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