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THZ1

THZ1

产品编号 T3664   CAS 1604810-83-4
别名: CDK7 inhibitor, THZ1 2HCl

THZ1 (CDK7 inhibitor) 是一种新型的选择性强效共价 CDK7 抑制剂。它还抑制CDK12和CDK13,并下调 MYC 表达。

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THZ1 Chemical Structure
THZ1, CAS 1604810-83-4
规格 价格/CNY 货期 数量
1 mg ¥ 287 现货
5 mg ¥ 629 现货
10 mg ¥ 1,178 现货
25 mg ¥ 2,470 现货
50 mg ¥ 2,820 现货
100 mg ¥ 4,180 现货
1 mL * 10 mM (in DMSO) ¥ 784 现货
产品目录号及名称: THZ1 (T3664)
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选择批次  
纯度: 99.27%
纯度: 99.12%
纯度: 95.09%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 THZ1 (CDK7 inhibitor) is a novel selective and potent covalent CDK7 inhibitor.
靶点活性 CDK7:3.2 nM
体外活性 THZ1 uses a unique mechanism, combining ATP-site and allosteric covalent binding, as a means of attaining potency and selectivity for CDK7. THZ1 irreversibly inhibits RNAPII CTD phosphorylation by covalently targeting a unique cysteine located outside the kinase domain of CDK7. THZ1, but not THZ1-R, completely inhibits the phosphorylation of the established intracellular CDK7 substrate RNAPII CTD at Ser?5 and Ser?7, with concurrent loss of Ser?2 phosphorylation at 250?nM in Jurkat cells. THZ1 exhibits strong antiproliferative effects across a broad range of cancer cell lines from various cancer types. In Jurkat cells, low-dose THZ1 has a profound effect on a small subset of genes, including the key regulator RUNX1, thus contributing to subsequent loss of the greater gene expression program and cell death[1]. THZ1 causes defects in Pol II(polymerase II) phosphorylation, co-transcriptional capping, promoter proximal pausing, and productive elongation[2].
体内活性 THZ1 reduces the proliferation of KOPTK1 T-ALL cells in a human xenograft mouse model. THZ1 is well tolerated at 10 mg/kg with no observable body weight loss or behavioural changes, suggesting that it causes no overt toxicity in the animals[1].
激酶实验 For kinase assays following immunoprecipitation of FLAG-CDK7 protein from HCT116 or FLAG-CDK12 from 293A cellular lysates, cells are first treated with THZ1, THZ1-R, or DMSO for 4 hrs at 37°C. Cells are then harvested by lysis in 50 mM Tris HCl pH 8.0, 150 mM NaCl, 1% NP-40, 5 mM EDTA, and protease/phosphatase cocktails. Exogenous CDK7 or CDK12 proteins are immunoprecipitated from cellular lysates using FLAG antibody- conjugated agarose beads. Precipitated proteins are washed with lysis buffer 6 times, followed by 2 washes with kinase buffer (40 mM Hepes pH 7.5, 150 mM NaCl, 10 mM MgCl2, 5% glycerol) and subjected to in vitro kinase assays at 30°C for 45 minutes using 1 μg of the large subunit of RNAPII (RPB1) as substrate and 25 μM ATP and 10 μCi of 32P ATP. Kinase assays using recombinant CDK7/TFIIH/MAT1 are conducted in the manner as described above using 25 ng of CAK complex per reaction. For kinase assays designed to test time-dependent inactivation of CDK7 kinase activity, CAK complex is pre-incubated with indicated concentrations of THZ1, THZ1-R, or DMSO in kinase buffer without ATP for 4 hrs at 30°C prior to being subjected to kinase assay conditions[1].
细胞实验 Cells are treated with THZ1, THZ1-R or dimethylsulphoxide (DMSO) for 0-6?h to assess the effect of time on the THZ1-mediated inhibition of RNAPII CTD phosphorylation. For subsequent experiments cells are treated with compounds for 4?h as determined by the time-course experiment described earlier, unless otherwise noted. For inhibitor washout experiments, cells are treated with THZ1, THZ1-R or DMSO for 4?h. Medium containing inhibitors is subsequently removed to effectively 'washout' the compound and the cells are allowed to grow in the absence of inhibitor. For each experiment, lysates are probed for RNAPII CTD phosphorylation and other specified proteins.(Only for Reference)
别名 CDK7 inhibitor, THZ1 2HCl
化合物与蛋白结合的复合物

T3664_1

Structure of the human CAK in complex with THZ1

分子量 566.05
分子式 C31H28ClN7O2
CAS No. 1604810-83-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 27 mg/mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Kwiatkowski N, et al. Nature. 2014, 511(7511):616-20. 2. Nilson KA, et al. Mol Cell. 2015, 59(4):576-87.

文献引用

1. Zhang G M, Huang S S, Ye L X, et al. Reciprocal positive regulation between BRD4 and YAP in GNAQ-mutant uveal melanoma cells confers sensitivity to BET inhibitors. Pharmacological Research. 2022: 106464. 2. Zhao F, Huang Y, Zhang Y, et al. SQLE inhibition suppresses the development of pancreatic ductal adenocarcinoma and enhances its sensitivity to chemotherapeutic agents in vitro. Molecular Biology Reports. 2022: 1-9
SEL120-34A CDK9-IN-7 TL12-186 Cirtuvivint Abemaciclib metabolite M2 CDKI-73 GSK 3 Inhibitor IX (R)-Enitociclib

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 神经退行性疾病化合物库 表型筛选靶点鉴定库 抑制剂库 经典已知活性库 抗衰老化合物库 抗胰腺癌化合物库 抗阿尔茨海默症化合物库 共价抑制剂库 已知活性化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

THZ1 1604810-83-4 Cell Cycle/Checkpoint CDK inhibit THZ-1 THZ 1 CDK7 inhibitor Cyclin dependent kinase Inhibitor THZ1 2HCl inhibitor

 

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