THAL SNS 032
Chemical Name: N-(5-(((5-(tert-Butyl)oxazol-2-yl)methyl)thio)thiazol-2-yl)-1-(14-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-2-oxo-6,9,12-trioxa-3-azatetradecyl)piperidine-4-carboxamide
Biological ActivityPROTAC comprising the cyclin-dependent kinase inhibitor SNS 032 (Cat. No. 4075) conjugated to the cereblon E3 ligase ligand, thalidomide (Cat. No. 0652). Potent, selective and cereblon-dependent degrader of CDK9 (EC50 = 4 nM). Displays >15-fold selectivity for CDK9 over other CDKs (EC50 values are 62, 171 and 398 nM for CDK2, CDK1 and CDK7, respectively). Induces complete degradation of CDK9 at 250 nM in MOLT4 cells. Inhibits proliferation of leukemia cell lines.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation.
Olson et al.
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