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THZ1
$106 – $825
Products Details
Product 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].
Web ID
– HY-80013
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C31H28ClN7O2
Citations
– 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. June 18, 2021.|Cancer Immunol Res. 2021 Apr 19.|Cancer Lett. 2021 Mar 16;S0304-3835(21)00117-8.|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.|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|Hepatology. 2019 Jun;69(6):2502-2517.|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. |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.|Proc Natl Acad Sci U S A. 2019 Jun 25;116(26):12986-12995. |Research Square Preprint. 2022 Feb.|Research Square Preprint. 2022 Jan.|Research Square Print. September 29th, 2022.|Sci Adv. 2020 Jul 17;6(29):eaba1593.|Science. 2021 Apr 30;372(6541):eaba8490.|TUMOR, 2017, 37(11): 1119-1127.|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.
References
– [1]Jiang YY, et al. Targeting super-enhancer-associated oncogenes in oesophageal squamous cell carcinoma. Gut. 2016 May 10. pii: gutjnl-2016-311818.|[2]Kwiatkowski N, et al. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014 Jul 31;511(7511):616-20.|[3]Zeng M, et al. Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13. Elife. 2018 Nov 13;7. pii: e39030.|[4]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.|[5]Chipumuro, et al. CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer. Cell. 2014 Nov 20;159(5):1126-39. ?
CAS Number
– 1604810-83-4
Molecular Weight
– 566.05
Compound Purity
– 99.84
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
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– DMSO : 100 mg/mL (ultrasonic)|Ethanol : 1.4 mg/mL (ultrasonic)
Target
– CDK
Isoform
– CDK12;CDK13;CDK7
Pathway
– Cell Cycle/DNA Damage
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
