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  • 化合物 Tubastatin A|T1966|TargetMol

化合物 Tubastatin A|T1966|TargetMol

Tubastatin A
1252003-15-8
287 10mg 起订
463 25mg 起订
672 50mg 起订
上海 更新日期:2024-09-29

TargetMol中国(陶术生物)

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产品详情:

中文名称:
化合物 Tubastatin A
英文名称:
Tubastatin A
CAS号:
1252003-15-8
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
99.51%
产品类别:
抑制剂
货号:
T1966

Product Introduction

Bioactivity

NameTubastatin A
DescriptionTubastatin A (Tubastatin A BASE) is an effective and specific HDAC6 inhibitor (IC50: 15 nM, in a cell-free assay). Its selectivity is 1000-fold against all the other isozymes except HDAC8.
Cell ResearchAnchorage-independent growth is assessed by growing cells in soft agar. About 25,000 cells suspended in 0.4% agar in culture media are layered over a 1% agar layer in a 6-well plate. Media are added twice a week and pictures are taken after 21 days of incubation. The number and size of colonies are analyzed using the Gel-Pro software.(Only for Reference)
Kinase AssayHDAC enzymatic assays: Tubastatin A is dissolved and diluted in assay buffer (50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, and 20 μM tris(2-carboxyethyl)phosphine) to 6-fold of the final concentration. HDAC enzymes are diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with Tubastatin A for 10 minutes before the addition of the substrate. The amount of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) used for each enzyme is equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 is diluted in assay buffer to 6-fold the final concentration with 0.3 μM sequencing grade trypsin. The substrate/trypsin mix is added to the enzyme/compound mix and the plate is shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction is monitored for release of 7-amino-4-methoxy-coumarin over 30 minutes, after deacetylation of the lysine side chain in the peptide substrate, and the linear rate of the reaction is calculated.
In vitro与对照组相比,Tubastatin A 可使PCNA阳性细胞的量显著降低(34% vs 65%).在同基因大鼠原位胆管癌模型中,Tubastatin A(10 mg/kg)降低瘤重与肝重和体重(分别为5和5.6倍)的比值.在给弗氏完全佐剂诱导的动物炎症模型中,Tubastat A(30 mg/kg,i.p.)对鼠爪体积有显著抑制作用.Tubastat A(30 mg/kg,i.p.)处理胶原诱导型关节炎DBA1小鼠的爪子组织,使临床评分(70%)和IL-6表达显著降低.
In vivoTubastatin A(5 μM)剂量依赖性地使神经元细胞免于同型半胱氨酸诱导的死亡,10 μM时可完全避免。 Tubastatin A(10 μM)对组蛋白乙酰化有轻微诱导作用。作用于胆管癌细胞系时,Tubastatin A(10 μM)促使乙酰化α-tubulin水平增加和初级纤毛表达的恢复,初级纤毛表达的恢复与Hedgehog、MAPK信号通路下调、细胞增殖率(平均50%)和浸润(40%)减少相关。作用于脂多糖刺激的人类 THP-1巨噬细胞时,Tubastatin A明显抑制TNF-α和IL-6(IC50:272/712 nM)。作用于小鼠Raw 264.7巨噬细胞时,Tubastatin A剂量依赖性抑制一氧化氮分泌(IC50:4.2 μM)。
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 35 mg/mL (104.35 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
KeywordsAutophagy | Inhibitor | Apoptosis | inhibit | HDAC | Histone deacetylases | Tubastatin A
Inhibitors RelatedGuanidine hydrochloride | Naringin | Taurine | Gefitinib | Hydroxychloroquine | 5-Fluorouracil | Curcumin | Stavudine | Tributyrin | L-Ascorbic acid | Paeonol | Sodium 4-phenylbutyrate
Related Compound LibrariesInhibitor Library | Bioactive Compound Library | Bioactive Compounds Library Max | Autophagy Compound Library | Apoptosis Compound Library | Anti-Aging Compound Library | Highly Selective Inhibitor Library | HIF-1 Signaling Pathway Compound Library | NF-κB Signaling Compound Library | Reprogramming Compound Library
Tubastatin A BASE|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

化合物 Tubastatin A相关厂家报价 更多

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