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THZ1

93 Cited Publications
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Based on 93 publication(s) in Google Scholar

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.

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  • Pureté: 98.43%
  • CAS No.: 1604810-83-4
  • Formule: C31H28ClN7O2
  • Masse moléculaire:566.05
  • Stockage:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 6 months , -20°C, 1 month
  • THZ1 Chemical Structure
    THZ1 Chemical Structure
  • Experimental Validation Results for THZ1
  • Experimental Validation Results for THZ1
  • Experimental Validation Results for THZ1
  • Experimental Validation Results for THZ1
  • Experimental Validation Results for THZ1
  • Experimental Validation Results for THZ1
  • Experimental Validation Results for THZ1
  • Experimental Validation Results for THZ1
  • Experimental Validation Results for THZ1
  • Experimental Validation Results for THZ1
  • Experimental Validation Results for THZ1
  • Experimental Validation Results for THZ1
CAS No.: 1604810-83-4
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  • THZ1 Chemical Structure
    THZ1 Chemical Structure
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    THZ1 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 Jun;40(6):814-822. [Abstract]

    Customer Validation
     The protein expression levels of the genes related to cell cycle and metabolism are detected by immunoblotting using the corresponding antibodies in H1299 cells treated with 20 nM THZ1 alone or in combination with 500 nM CB-839 for 48 h.

  • 1/16

    THZ1 purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 May;38(20):3932-3945. [Abstract]

    Customer Validation
     Immunoblot analysis of the MYC and β-actin in cells (MiaPaCa2 and MiaPaCa2-R) treated with the indicated dose of THZ1 for 6 h.

  • 1/16

    THZ1 purchased from MedChemExpress. Usage Cited in: Onco Targets Ther. 2019 Mar 22:12:2137-2147. [Abstract]

    Customer Validation
     Western blot is used to assess the RNA Pol II protein and its phosphorylation at serine 2, serine 5, and serine 7 in cervical cancer cells after treatment with the indicated concentrations of THZ1.

  • 1/16

    THZ1 purchased from MedChemExpress. Usage Cited in: Cell. 2018 Sep 20;175(1):171-185.e25. [Abstract]

    Customer Validation
     WB analysis of MV4-11 cells treated with BTX161 (6 hr), iCDK9 (4 hr), or THZ1 (4 hr) at the indicated concentrations in different combinations as indicated. PP2Ac is a loading control.

  • 1/16

    THZ1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Aug 23;9(1):3392. [Abstract]

    Customer Validation
     21mers are synthesized in parallel reactions with unlabeled (upper panel) or radiolabeled (lower panel) ribonucleoside triphosphates in the presence of DMSO (-) or increasing amounts of THZ1; reactions are stopped after 15 or 60 min.

  • 1/16

    THZ1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Nov 19;9(1):4866. [Abstract]

    Customer Validation
     MYCN, PHOX2B, and TBX2 protein levels 10 h and 16 h upon treatment with 1 μM JQ1, 35 nM THZ1 and the combination of JQ1 and THZ1 in the IMR-5/75 cell line.

  • 1/16

    THZ1 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Sep;16(9):1739-1750. [Abstract]

    Customer Validation
     Western blot analysis of RNAPII CTD phosphorylation in ovarian cancer cells that are treated with THZ1.

  • 1/16

    THZ1 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Sep;16(9):1739-1750. [Abstract]

    Customer Validation
     Western blot analysis of RNAPII CTD phosphorylation in ovarian cancer cells that are treated with THZ1.

  • 1/16

    THZ1 purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Sep;16(9):1739-1750. [Abstract]

    Customer Validation
     Western blot analysis of RNAPII CTD phosphorylation in ovarian cancer cells that are treated with THZ1.

  • 1/16

    THZ1 purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2017 May 15;6(5):e336. [Abstract]

    Customer Validation
     Lysates from cells treated with vehicle or 200 nM THZ1 for 48 h analyzed for the activation status of multiple CDKs as indicated to the right of panels by western blotting.

  • 1/16

    THZ1 purchased from MedChemExpress. Usage Cited in: TUMOR, 2017, 37(11): 1119-1127.

    Customer Validation
     The expression level of cyclin-dependent kinase 7 (CDK7) and the phosphorylation level of RNA polymeraseⅡ carboxyl-terminal domain Ser-5 (RNAPolⅡS5) in ovarian cancer cells treated with THZ1 are detected by Western blotting. After the ovarian cancer IGROV1, OVCA433, SKOV3 and COV413B cells are treated with 0.5 μM THZ1 for 0, 4, 8, 12 and 24 h, the CDK7 expression and RNAPolⅡS5 phosphorylation levels are significantly down-regulated.

  • 1/16

    THZ1 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Apr 18;8(16):27353-27363. [Abstract]

    Customer Validation
     Representative Western blot showing the phosphorylation status of ERα at serine 118 (S118) in MCF-7 cells in controls and after treatment with the CDK7 inhibitor, THZ1 (100 nM), or AG-490 (100 μM) for 3 h prior to E2 treatment for 30 min. Endogenous ERα and β-actin are used as loading controls.

  • THZ1