For research use only.

Catalog No.S7549

17 publications

THZ1 2HCl Chemical Structure

CAS No. 1604810-83-4(freebase)

THZ1 is a covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7.

Selleck's THZ1 2HCl has been cited by 17 publications

1 Customer Review

  • One and three days after differentiation induction, protein level of Myh3 and Myogenin were analyzed by western blot.

    J Cancer, 2018, 9(17):3149-3155. THZ1 2HCl purchased from Selleck.

Purity & Quality Control

Choose Selective CDK Inhibitors

Biological Activity

Description THZ1 is a covalent CDK7 inhibitor which has the unprecedented ability to target a remote cysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity for CDK7.
CDK7 [1]
(Cell-based assay)
3.2 nM
In vitro

THZ1 uses a unique mechanism, combining ATP-site and allosteric covalent binding, as a means of attaining potency and selectivity for CDK7. THZ1 irreversibly inhibits RNAPII CTD phosphorylation by covalently targeting a unique cysteine located outside the kinase domain of CDK7. THZ1, but not THZ1-R, completely inhibits the phosphorylation of the established intracellular CDK7 substrate RNAPII CTD at Ser 5 and Ser 7, with concurrent loss of Ser 2 phosphorylation at 250 nM in Jurkat cells. THZ1 exhibits strong antiproliferative effects across a broad range of cancer cell lines from various cancer types. In Jurkat cells, low-dose THZ1 has a profound effect on a small subset of genes, including the key regulator RUNX1, thus contributing to subsequent loss of the greater gene expression program and cell death[1]. THZ1 causes defects in Pol II(polymerase II) phosphorylation, co-transcriptional capping, promoter proximal pausing, and productive elongation[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Jurkat cells NW\mOJdjS3m2b4TvfIlkcXS7IHHzd4F6 MVu3NkBp M3;CcWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGp2emujdDDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhemW|YYr1dolvKGG|c3H5MEBKSzVyPUCuNFUh|ryP M{Pkd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG1OVcyLz5{NkGxOVU4OTxxYU6=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
pS2 / pS5 / pS7 / RNAPII / MYCN / MCL-1 / Cleaved PARP; 

PubMed: 29276047     

Western blot (WB) analysis of the indicated proteins in THZ1S and THZ1R cells treated with DMSO or THZ1 (right) (Kelly, 1 μM; NGP, LAN5, SK-N-BE2 [BE2], 300 nM) for 6 hr.

KLF5 / FGFBP / c-MYC ; 

PubMed: 31360115     

HCC1806 and HCC1937 cells were treated with THZ1 for 24 h. The KLF5, FGFBP and c-MYC protein levels were detected by immunoblotting. THZ1 is a CDK7 inhibitor. 

RNP2-p-Ser2 / RNP2-p-Ser5 / RNP2-p-Ser7 / CDK7 ; 

PubMed: 31399555     

HuCCT1, RBE, and HuH28 cells were treated with THZ1 at a concentration of 200 nM for 3, 6, 12, and 24 h. RNP2 and RNP2 phosphorylation were analyzed by western blotting.

29276047 31360115 31399555
Growth inhibition assay
Cell viability; 

PubMed: 31399555     

Five CCA cell lines (HuCCT1, HuH28, RBE, HCCC9810, and OZ) were plated in 96-well plates and treated with THZ1 or THZ1R (a THZ1 analog with no significant inhibitory activity of CDK7) at different concentrations for 72 h. Cell viability was measured by CCK-8 assay and dose–response curves show percent cell viability to that of DMSO-treated cells. IC50 values were calculated using nonlinear regression analysis in Prism 7.0. Data represent mean ± SEM of three independent replicates.

In vivo THZ1 reduces the proliferation of KOPTK1 T-ALL cells in a human xenograft mouse model. THZ1 is well tolerated at 10 mg/kg with no observable body weight loss or behavioural changes, suggesting that it causes no overt toxicity in the animals[1].


Cell Research:[1]
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  • Cell lines: Jurkat, Loucy, KOPTK1 and DND-41 cell lines
  • Concentrations: 0-10 μM
  • Incubation Time: 4 h
  • Method: Cells are treated with THZ1, THZ1-R or dimethylsulphoxide (DMSO) for 0-6 h to assess the effect of time on the THZ1-mediated inhibition of RNAPII CTD phosphorylation. For subsequent experiments cells are treated with compounds for 4 h as determined by the time-course experiment described earlier, unless otherwise noted. For inhibitor washout experiments, cells are treated with THZ1, THZ1-R or DMSO for 4 h. Medium containing inhibitors is subsequently removed to effectively 'washout' the compound and the cells are allowed to grow in the absence of inhibitor. For each experiment, lysates are probed for RNAPII CTD phosphorylation and other specified proteins.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: Bioluminescent xenografted mouse model
  • Dosages: 10 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (156.5 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+45% PEG 300+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 638.97


CAS No. 1604810-83-4(freebase)
Storage powder
in solvent
Synonyms N/A
Smiles CN(C)CC=CC(=O)NC1=CC=C(C=C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)C4=CNC5=CC=CC=C54)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O

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CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID