THZ1

• Description :

  THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression[1][2].

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  CDK

• Type :

  Reference compound

• Related Pathways :

  Cell Cycle/DNA Damage

• Applications :

  Cancer-Kinase/protease

• Field of Research :

  Cancer

• Assay Protocol :

  https://www.medchemexpress.com/THZ1.html

• Purity :

  99.84

• Solubility :

  DMSO : 100 mg/mL (ultrasonic)

• Smiles :

  ClC1=CN=C(NC2=CC(NC(C3=CC=C(NC(/C=C/CN(C)C)=O)C=C3)=O)=CC=C2)N=C1C4=CNC5=CC=CC=C54

• Molecular Formula :

  C31H28ClN7O2

• Molecular Weight :

  566.05

• Precautions :

  H302, H315, H319, H335

• References & Citations :

  [1]Kwiatkowski N, et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014 Jul 31;511 (7511) :616-20.|[2]Zeng M, et al. Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13. Elife. 2018 Nov 13;7. pii: e39030.|[3]Christensen CL, et al. Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor. Cancer Cell. 2014 Dec 8;26 (6) :909-22.|[4]Chipumuro, et al. CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer. Cell. 2014 Nov 20;159 (5) :1126-39. ?|[5]Jiang YY, et al. Targeting super-enhancer-associated oncogenes in oesophageal squamous cell carcinoma. Gut. 2016 May 10. pii: gutjnl-2016-311818.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  CDK12; CDK13; CDK7

• Citation 01 :

  Acta Pharmacol Sin. 2019 Jun;40 (6) :814-822.|Autophagy. 2021 Jun;17 (6) :1426-1447.|Biochem Biophys Res Commun. 2023 Dec 31:689:149188.|Biochim Biophys Acta Mol Cell Res. 2019 Jun;1866 (6) :978-991.|bioRxiv. 2019 Oct. |bioRxiv. 2024 July 12.|bioRxiv. 2024 July 27.|bioRxiv. 2025 Aug 19.|bioRxiv. June 18, 2021.|Cancer Immunol Res. 2021 Jun;9 (6) :707-722.|Cancer Lett. 2021 Jun 1:507:70-79.|Cancer Lett. 2024 May 1:589:216811.|Cancer Res. 2021 Jun 1;81 (11) :3105-3120.|Cancer Res. 2025 May 14.|Cancers (Basel) . 2022 Jun 1;14 (11) :2755.|Cell Chem Biol. 2025 Apr 17;32 (4) :556-569.e24.|Cell Commun Signal. 2022 Sep 5;20 (1) :96.|Cell Death Differ. 2023 May;30 (5) :1260-1278.|Cell Death Dis. 2020 Sep 15;11 (9) :754.|Cell Death Dis. 2021 Aug 3;12 (8) :763.|Cell Death Dis. 2021 Mar 3;12 (3) :229.|Cell Death Dis. 2019 Aug 9;10 (8) :602.|Cell Oncol (Dordr) . 2021 Aug;44 (4) :871-887.|Cell Rep Med. 2023 Apr 18;4 (4) :101007.|Cell Rep. 2022 Apr 26;39 (4) :110732.|Cell. 2017 Sep 7;170 (6) :1209-1223.e20. |Cell. 2018 Sep 20;175 (1) :171-185.e25.|Cells. 2019 Oct 6;8 (10) :1208.|Cells. 2020 Mar 6;9 (3) :638.|Cells. 2021 May 12;10 (5) :1182.|Cells. 2020 Mar 4;9 (3) :621. |Chin Med J (Engl) . 2022 Oct 20;135 (20) :2436-2445.|Clin Cancer Res. 2019 Oct 15;25 (20) :6195-6205.|EMBO Mol Med. 2022 Apr 7;14 (4) :e14990.|Eur J Pharmacol. 2023 Sep 15:955:175892.|FEBS J. 2024 May 11.|Front Mol Biosci. 2021 Aug 19;8:697457.|Front Oncol. 2021 May 24;11:664848.|Genes Dev. 2020 Jan 1;34 (1-2) :53-71. |Harvard Medical School LINCS LIBRARY|Heliyon. 2024 Jan 9;10 (2) :e24389.|Hepatology. 2019 Jun;69 (6) :2502-2517.|iScience. 2024 May 16.|IUBMB Life. 2021 Dec;73 (12) :1446-1459.|J Exp Clin Cancer Res. 2021 Apr 26;40 (1) :141.|J Exp Clin Cancer Res. 2022 Aug 10;41 (1) :241.|J Exp Clin Cancer Res. 2022 Oct 22;41 (1) :311.|J Exp Clin Cancer Res. 2023 Aug 21;42 (1) :214.|J Invest Dermatol. 2021 Nov;141 (11) :2656-2667.e11.|J Med Chem. 2022 Dec 8;65 (23) :15770-15788.|J Mol Neurosci. 2022 Feb;72 (2) :410-419.|mBio. 2025 Dec 10;16 (12) :e0289825.|Mol Cancer Ther. 2017 Sep;16 (9) :1739-1750. |Nat Cell Biol. 2020 Oct;22 (10) :1187-1196.|Nat Commun. 2019 Jul 25;10 (1) :3319. |Nat Commun. 2024 Aug 9;15 (1) :6810.|Nat Commun. 2025 Feb 2;16 (1) :1271.|Onco Targets Ther. 2019 Mar 22:12:2137-2147.|Oncogene. 2019 May;38 (20) :3932-3945. |Oncogene. 2022 Sep;41 (40) :4524-4536.|Oncogenesis. 2017 May 15;6 (5) :e336.|Oncogenesis. 2020 May 12;9 (5) :47.|PLoS Pathog. 2024 Apr 19;20 (4) :e1012138.|PLoS Pathog. 2025 Nov 11;21 (11) :e1013694.|Proc Natl Acad Sci U S A. 2019 Jun 25;116 (26) :12986-12995. |Regen Biomater. 2024 Mar 1:11:rbae020.|Res Sq. 2025 Apr 24:rs.3.rs-6506954.|Research Square Preprint. 2022 Feb.|Research Square Preprint. 2022 Jan.|Research Square Print. September 29th, 2022.|Sci Adv. 2020 Jul 17;6 (29) :eaba1593.|Sci Rep. 2024 May 8;14 (1) :10582.|Science. 2021 Apr 30;372 (6541) :eaba8490.|TUMOR, 2017, 37 (11) : 1119-1127.|Universidade de Lisboa. 2021 Dec 21.|University of London. 2022 May.|Breast Cancer Res. 2023 May 5;25 (1) :51.|Cancer Discov. 2019 Nov;9 (11) :1538-1555.|Drug Dev Res. 2025 Feb;86 (1) :e70049.|Front Oncol. 2021 Apr 6:11:663360.|Harvard Medical School LINCS LIBRARY|Int J Biol Sci. 2019 Jun 10;15 (8) :1733-1742.|Mol Cell. 2019 May 16;74 (4) :674-687.e11.|Nat Commun. 2018 Nov 19;9 (1) :4866.|Nat Commun. 2018 Aug 23;9 (1) :3392.|Nat Med. 2019 Feb;25 (2) :292-300.|Oncotarget. 2017 Apr 18;8 (16) :27353-27363.|Patent. US20220288067A1.|Research Square Print. 2022 May.

• CAS Number :

  [1604810-83-4]