THZ1

• UNSPSC 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].

• Target Antigen:

  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)|Ethanol : < 1 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 Weight:

  566.05

• 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.Acta Pharmacol Sin. 2019 Jun;40(6):814-822.|Autophagy. 2021 Jun;17(6):1426-1447.|Biochem Biophys Res Commun. 2023 Nov 7, 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. June 18, 2021.|Cancer Immunol Res. 2021 Apr 19.|Cancer Lett. 2021 Mar 16;S0304-3835(21)00117-8.|Cancer Lett. 2024 Mar 13:216811.|Cancer Res. 2021 Jun 1;81(11):3105-3120.|Cancers (Basel). 2022, 14(11), 2755.|Cell Commun Signal. 2022 Sep 5;20(1):96.|Cell Death Differ. 2023 Feb 24.|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. 2021 Apr 27.|Cell Rep Med. 2023 Mar 31;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. |Chinese Medical Journal. 2022.|Clin Cancer Res. 2019 Oct 15;25(20):6195-6205.|EMBO Mol Med. 2022 Mar 7;e14990.|Eur J Pharmacol. 2023 Jul 8;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.|Hepatology. 2019 Jun;69(6):2502-2517.|iScience. 2024 May 16.|IUBMB Life. 2021 Oct 30.|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 May 15;S0022-202X(21)01232-X.|J Med Chem. 2022 Nov 17.|J Mol Neurosci. 2021 Aug 31.|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.|Onco Targets Ther. 2019 Mar 22;12:2137-2147. |Oncogene. 2019 May;38(20):3932-3945. |Oncogene. 2022 Aug 30.|Oncogenesis. 2017 May 15;6(5):e336.|Oncogenesis. 2020 May 12;9(5):47.|PLoS Pathog. 2024 Apr 19;20(4):e1012138.|Proc Natl Acad Sci U S A. 2019 Jun 25;116(26):12986-12995. |Regen Biomater. 2024 Mar 1.|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.|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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

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

• Clinical Information:

  No Development Reported

• CAS Number:

  1604810-83-4