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THZ1-R

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Catalog No. T13153Cas No. 1621523-07-6
Alias THZ1R

THZ1-R is a non-covalent active analogue of THZ1, with the acrylamide group removed from THZ1, losing its ability to covalently bind to the C312 cysteine residue of CDK7. Its CDK7 inhibitory activity is weaker than that of THZ1.

THZ1-R

THZ1-R

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Catalog No. T13153Alias THZ1RCas No. 1621523-07-6
THZ1-R is a non-covalent active analogue of THZ1, with the acrylamide group removed from THZ1, losing its ability to covalently bind to the C312 cysteine residue of CDK7. Its CDK7 inhibitory activity is weaker than that of THZ1.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$499-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Appearance:Viscous
Color:Yellow
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Product Introduction

Bioactivity
Description
THZ1-R is a non-covalent active analogue of THZ1, with the acrylamide group removed from THZ1, losing its ability to covalently bind to the C312 cysteine residue of CDK7. Its CDK7 inhibitory activity is weaker than that of THZ1.
Targets&IC50
CDK7:146 nM
In vitro
Method:
Loucy cells were treated with varying concentrations of THZ1 or 10 µM THZ1-R for 4 hours. Cell lysates were then incubated with bio-THZ1, followed by immunoblotting and immunoprecipitation to detect CDK7 labeling and competitive binding.

Result:
Bio-THZ1 effectively pulled down CDK7, and THZ1 competed for binding in a dose-dependent manner. Immunoprecipitation confirmed that bio-THZ1 specifically labels CDK7, indicating that THZ1 covalently binds to intracellular CDK7. [1]
SynonymsTHZ1R
Chemical Properties
Molecular Weight568.07
FormulaC31H30ClN7O2
Cas No.1621523-07-6
SmilesO=C(NC=1C=CC=C(C1)NC=2N=CC(Cl)=C(N2)C3=CNC=4C=CC=CC43)C5=CC=C(C=C5)NC(=O)CCCN(C)C
Relative Density.1.362 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 80 mg/mL (140.83 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble)
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (5.81 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7603 mL8.8017 mL17.6035 mL88.0173 mL
5 mM0.3521 mL1.7603 mL3.5207 mL17.6035 mL
10 mM0.1760 mL0.8802 mL1.7603 mL8.8017 mL
20 mM0.0880 mL0.4401 mL0.8802 mL4.4009 mL
50 mM0.0352 mL0.1760 mL0.3521 mL1.7603 mL
100 mM0.0176 mL0.0880 mL0.1760 mL0.8802 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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