THZ1 is a novel selective and potent covalent CDK7 inhibitor with IC50(binding affinity) of 3.2 nM; inhibits Jurkat cell's proliferation with IC50 of 50 nM.
IC50 value: 3.2 nM (Kd For CDK7)
Target: CDK7
THZ1 Hydrochloride has the unprecedented ability to target a remotecysteine residue located outside of the canonical kinase domain, providing an unanticipated means of achieving selectivity For CDK7.
Cancer cell-line profiling indicates that a subset of cancer cell lines,
including human T-cell acute lymphoblastic leukaemia (T-ALL), have exceptional sensitivity to THZ1 Hydrochloride. Genome-wide analysis in Jurkat T-ALL cells shows thatTHZ1 Hydrochloride disproportionally affects transcription of RUNX1 and suggests that sensitivity to THZ1 Hydrochloride may be due to vulnerability conferred by the RUNX1 super-enhancer and the key role of RUNX1 in the core transcriptional regulatory circuitry of these tumour cells.
Pharmacological modulation of CDK7 kinase activity may thus provide an approach toidentify and treat tumour types that are dependent on transcription For maintenance of the oncogenic state.For the detailed information of THZ1 Hydrochloride, the solubility of THZ1 Hydrochloride in water, the solubility of THZ1 Hydrochloride in DMSO, the solubility of THZ1 Hydrochloride in PBS buffer, the animal experiment (test) of THZ1 Hydrochloride, the cell expriment (test) of THZ1 Hydrochloride, the in vivo, in vitro and clinical trial test of THZ1 Hydrochloride, the EC50, IC50,and Affinity of THZ1 Hydrochloride, Please contact DC Chemicals.
