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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 Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $346 | 6-8 weeks | |
5 mg | $497 | In Stock | |
25 mg | $1,543 | 6-8 weeks | |
50 mg | Inquiry | 6-8 weeks | |
100 mg | Inquiry | 6-8 weeks | |
1 mL x 10 mM (in DMSO) | $547 | 6-8 weeks |
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] |
Synonyms | THZ1R |
Molecular Weight | 568.07 |
Formula | C31H30ClN7O2 |
Cas No. | 1621523-07-6 |
Smiles | O=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 | store 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) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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