TH-Z827 CAS No.: 2847881-81-4

Chemical Structure : TH-Z827

CAS No.: 2847881-81-4

 

TH-Z827

Catalog No.: URK-V2498 Only Used For Lab.

TH-Z827 is a potent and selective inhibitor of the cyclin-dependent kinase 7(CDK7).

Biological Activity

TH-Z827 (CAS No.: 2847881-81-4) is a potent and selective inhibitor of the cyclin-dependent kinase 7(CDK7).
Cyclin-dependent kinase 7 (CDK7) plays a critical role in transcriptional regulation by phosphorylating the RNA polymerase II(C-terminal domain). CDK7 is also an essential component of the CDK-activating kinase (CAK) complex, which activates other CDKs and regulates the cell cycle. Whereas CDK7 inhibitors potentially exert selective toxicity against tumor cells, take advantage of the increased dependence of cancer cells on CDK7-mediated transcription.
CDK7 binds to cyclins H and Mat1 to form CAK, which can phosphorylate and activate other CDKs. TH-Z827 functions as a competitive ATP-competitive inhibitor of CDK7, binding to the ATP-binding pocket to block the CDK7 activation process. TH-Z827 has high potency against CDK7, selectivity, and enzyme inhibition.
TH-Z827 has shown excellent potential to treat human cancer in different models and is being developed as a clinical candidate by Beijing Hua Medicine Ltd., a Chinese pharmaceutical company. many preclinical studies are developing specifically targeting human cancers. The phase I clinical trial for TH-Z827 is ongoing in China.
TH-Z827 is a potent and selective inhibitor of CDK7, which plays a vital role in transcriptional regulation and cell cycle regulation. TH-Z827 has high potency, selectivity, and enzyme inhibition.

Physicochemical Properties

References

1. Bartkowiak, B., Yan, C., Greenleaf, A. et al. CDK Subunit Altered Expression Is Revealed in Human Cancer Cell Lines.

2. Chao, S. H. Mechanisms of CDK7 inhibitor induced transcriptional repression in osteosarcoma cells.

3. Jiang, B., Yan, C., Li, C., et al. Discovery of 3-(2-(pyridin-4-yl)thiazol-4-ylamino)benzoic acid derivatives as potent, selective, and orally bioavailable inhibitors of cyclin-dependent kinase 7.

4. Zhang, Y., Zhang, T., Wan, Y., et al. A novel orally available inhibitor of cyclin-dependent kinase 7 (CDK7) reveals determinants of inhibitor potency.

URK-V2498_COA

URk-V2498_SDS

URK-V2498_TDS

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