Catalog No. A8882

THZ1

CDK7共价抑制剂

规格	价格	货期
1mL(10 mM in DMSO)	￥818.00	现货
5mg	￥681.00	现货
10mg	￥1227.00	现货
25mg	￥2727.00	现货

CAS号：1604810-83-4纯度：96.87%

仅用于科研，不用于诊疗。未经明确授权不得转售。

021-55669583sales@apexbio.cnAPExBIO

特色产品

Annexin V-FITC/PI Apoptosis Kit

用于双染检测细胞凋亡和坏死

- 在10-20分钟内完成染色
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞

Phos binding reagent (Phosbind) acrylamide

分离和检测磷酸化/非磷酸化蛋白

- 新型的磷酸盐结合标签和功能分子
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白

Cell Counting Kit-8 (CCK-8)

用于细胞增殖和细胞毒性试验

- 比MTT，MTS或WST-1更敏感
- 对细胞无毒性
- 步骤更简单，无需有机溶剂

Cy5 TSA Fluorescence System Kit

Cy5荧光标记的酪胺信号放大系统

- 检测ICC/IHC/ISH中的低丰度靶点
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率

EZ Cap™ Cy5 Firefly Luciferase mRNA (5-moUTP)

用于观察mRNA运送，定位，翻译

- 具有Cap1结构的荧光素酶mRNA
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰

HotStart™ 2X Green qPCR Master Mix

用于荧光定量目标DNA或cDNA

- 通过热启动机制优化扩增特异性
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单

HyperScribe™ T7 High Yield Cy5 RNA Labeling Kit Plus

高效的Cy5修饰RNA转录试剂盒

- 适合原位/Northernblot杂交实验
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量

产品描述产品性质产品应用生物相关数据质量控制操作说明产品引用文献摩尔浓度计算器

产品描述

THZ1是一种CDK7的共价抑制剂，IC50值为3.2 nM。

THZ1能够靶向共价修饰CDK7激酶结构域外的C312残基。在激酶结合试验中，THZ1表现出良好的亲和性，IC50值为3.2 nM。THZ1可以有效地抑制Jurkat和Loucy T-ALL细胞的生长，IC50值分别为50 nM和0.55 nM。据报道，THZ1在Jurkat和Loucy细胞中扰乱CDK7信号通路。针对各种癌细胞系，THZ1展示了低于200 nM的IC50值的广泛活性。在这些细胞系中，T-ALL对THZ1表现出了特殊的敏感性，这是由于THZ1引起的RUNX1的转录效应。

作为CDK7的抑制剂，THZ1可以抑制CDK蛋白的激活。THZ1也可以抑制RNA聚合酶II的C-末端结构域的磷酸化，从而影响转录调控。

参考文献：
[1] Nicholas Kwiatkowski, Tinghu Zhang, Peter B. Rahl et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature, 2014.

产品性质

物理外观	Solid
CAS号	1604810-83-4
分子式	C₃₁H₂₈ClN₇O₂
分子量	566.05
化学名称	(E)-N-(3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)-4-(4-(dimethylamino)but-2-enamido)benzamide
溶解度	≥28.3 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
SMILES	ClC1=CN=C(N=C1C2=CNC3=CC=CC=C23)NC4=CC=CC(NC(C5=CC=C(NC(/C=C/CN(C)C)=O)C=C5)=O)=C4
存储条件	-20°C
运输条件	蓝冰

产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)

IC50和靶点

生物活性描述	THZ1是一种不可逆的；有效的和选择性的CDK7（细胞周期蛋白依赖性激酶7）抑制剂。IC50为3.2 nM。
靶点	CDK7
生物活性数据	3.2 nM

生物相关数据

质量控制

请选择批次查看:

纯度 = 96.87%

NMR (Nuclear Magnetic Resonance)COA (Certificate Of Analysis)HPLC (Retest)MSDS (Material Safety Data Sheet)

操作说明

小分子化合物通用使用指南 Datasheet

APExBIO 顾客使用本产品发表的 26 篇科研文献

1. Dejan Mesner, Matthew V. X. Whelan, et al. "HIV-1 signalling remodels nuclear pores to licence infection." Nature. 2026 May 6. PMID: 42092137

2. Mai-Phuong Nguyen, Kaoru Yamagata, et al. "Pivotal contribution of super-enhancer-driven KLF6 expression to the adipogenesis of human adipose-derived stem cells." Inflamm Regen. 2026 Jan 19;46(1):5. PMID: 41549316

3. Chun-Fui Lai, Victoria I Cushing, et al. "Resistance to CDK7 inhibitors directed by acquired mutation of a conserved residue in cancer cells." EMBO J. 2025 Oct;44(20):5860-5889. PMID: 40921851

4. Yi Sui, Teng Wang, et al. "Targeting Super-Enhancer-Driven Transcriptional Dependencies Suppresses Aberrant Hedgehog Pathway Activation and Overcomes Smoothened Inhibitor." Cancer Res. 2024 May 22. PMID: 38775809

5. Roberta Cacioppo, Alexander Gillis, et al. "CRL3ARMC5 ubiquitin ligase and Integrator phosphatase form parallel mechanisms to control early stages of RNA Pol II transcription." Article Volume 84, Issue 24, p4808-4823.e13, December 19, 2024

6. Xavier Rambout, Hana Cho, et al. "PGC-1α senses the CBC of pre-mRNA to dictate the fate of promoter-proximally paused RNAPII." Mol Cell. 2023 January 19; 83(2): 186–202.e11. PMID: 36669479

7. Anh Phuong Nguyen, Kaoru Yamagata, et al. "Enhancer RNA commits osteogenesis via microRNA-3129 expression in human bone marrow-derived mesenchymal stem cells." Inflamm Regen. 2022 Sep 16;42(1):43. PMID: 36114571

8. Te Zhang, Xuming Song, et al. "Aberrant super-enhancer landscape reveals core transcriptional regulatory circuitry in lung adenocarcinoma." Oncogenesis. 2020 Oct 17;9(10):92. PMID: 33070167

9. Cho YS, Li S, et al. "CDK7 regulates organ size and tumor growth by safeguarding the Hippo pathway effector Yki/Yap/Taz in the nucleus." Genes Dev. 2020 Jan 1;34(1-2):53-71. PMID: 31857346

10. Kim J, Cho YJ, et al. "CDK7 is a reliable prognostic factor and novel therapeutic target in epithelial ovarian cancer." Gynecol Oncol. 2019 Nov 24. pii: S0090-8258(19)31625-7. PMID: 31776040

11. Shaj K, Hutcherson RJ, et al. "ATR Kinase Activity Limits Mutagenesis and Promotes the Clonogenic Survival of Quiescent Human Keratinocytes Exposed to UVB Radiation." Photochem Photobiol. 2019 Sep 25. PMID: 31554014

12. Sava GP, Fan H, et al. "ABC-transporter upregulation mediates resistance to the CDK7 inhibitors THZ1 and ICEC0942." Oncogene. 2019 Sep 17. PMID: 31530935

13. Seoane M, Buhs S, et al. "Lineage-specific control of TFIIH by MITF determines transcriptional homeostasis and DNA repair." Oncogene. 2019 Jan 16. PMID: 30651597

14. Maritere Urioistegui-Arcos, Rodrigo Aguayo-Ortiz, et al. "Disruption of TFIIH activities generates a stress gene expression response and reveals possible new targets against cancer." bioRxiv. 2019 December 03

15. KAVYA SHAJ. "DIFFERING FUNCTIONS OF ATR KINASE IN HUMAN EPIDERMAL KERATINOCYTES EXPOSED TO ULTRAVIOLET B RADIATION." Wright State University. 2019

16. Landsverk HB, Sandquist LE, et al. "Regulation of ATR activity via the RNA polymerase II associated factors CDC73 and PNUTS-PP1." Nucleic Acids Res. 2018 Dec 12. PMID: 30541148

17. Lin L, Huang M, et al. "Super-enhancer-associated MEIS1 promotes transcriptional dysregulation in Ewing sarcoma in co-operation with EWS-FLI1." Nucleic Acids Res. 2018 Nov 28. PMID: 30496486

18. Zanconato F, Battilana G, et al. "Transcriptional addiction in cancer cells is mediated by YAP/TAZ through BRD4." Nat Med. 2018 Oct;24(10):1599-1610. PMID: 30224758

19. Chen D, Zhao Z, et al. "Super enhancer inhibitors suppress MYC driven transcriptional amplification and tumor progression in osteosarcoma." Bone Res. 2018 Apr 4;6:11. PMID: 29644114

20. Tuzlak S, Haschka MD, et al. "Differential effects of Vav-promoter-driven overexpression of BCLX and BFL1 on lymphocyte survival and B cell lymphomagenesis." FEBS J. 2018 Apr;285(8):1403-1418. PMID: 29498802

21. Yuan J, Jiang YY, et al. "Super-Enhancers Promote Transcriptional Dysregulation in Nasopharyngeal Carcinoma." Cancer Res. 2017 Dec1;77(23):6614-6626. PMID: 28951465

22. Kemp MG. "DNA damage-induced ATR kinase activation in non-replicating cells is regulated by the XPB subunit of transcription factor II-H (TFIIH)." J Biol Chem. 2017 Jun 7. pii: jbc.M117.788406. PMID: 28592488

23. Liao R, Mizzen CA. "Site-specific regulation of histone H1 phosphorylation in pluripotent cell differentiation." Epigenetics Chromatin. 2017 May 22;10:29. PMID: 28539972

24. Francavilla C, Lupia M, et al. "Phosphoproteomics of Primary Cells Reveals Druggable Kinase Signatures in Ovarian Cancer." Cell Rep. 2017 Mar 28;18(13):3242-3256. PMID: 28355574

25. Posternak V, Ung MH, et al. "MYC Mediates mRNA Cap Methylation of Canonical Wnt/β-Catenin Signaling Transcripts By Recruiting CDK7 and RNA Methyltransferase." Mol Cancer Res. 2017 Feb;15(2):213-224. PMID: 27899423

26. Harrod A, Fulton J, et al. "Genomic modelling of the ESR1 Y537S mutation for evaluating function and new therapeutic approaches for metastatic breast cancer." Oncogene. 2017 Apr 20;36(16):2286-2296. PMID: 27748765

摩尔浓度计算器

质量

= 浓度

x 体积

x 分子量

*在配置溶液时，请务必参考产品标签上、MSDS / COA（可在Apexbio的产品页面获得）批次特异的分子量使用本工具。

THZ1

CDK7共价抑制剂

特色产品

产品描述

产品性质

产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)

IC50和靶点

生物相关数据

质量控制

操作说明

APExBIO 顾客使用本产品发表的 26 篇科研文献

摩尔浓度计算器

相关产品

THZ1

CDK7共价抑制剂

特色产品

产品描述

产品性质

产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)

IC50和靶点

生物相关数据

质量控制

操作说明

APExBIO 顾客使用本产品发表的 26 篇科研文献

摩尔浓度计算器

相关产品