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 ActivityTHAL SNS 032 is a degrader (PROTAC®) 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.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Application of THAL SNS 032 in MOLT-4 cells. Western Blot data showing knockdown of both CDK9 isoforms after THAL SNS 032 treatment of MOLT-4 cells (4 h incubation). Protein quantification (relative to DMSO-only control) is shown beneath the corresponding lane. Cdk9 primary antibody is used at 1:1000 dilution. Secondary is Anti-Rabbit HAF008, 1:1000, R&D Systems. GAPDH primary antibody is R&D Systems AF5718 used at 5μg/mL. Secondary is Anti-Goat HAF017, 1:1000, R&D Systems.Data courtesy of Jeff Cooper, Bio-Techne.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation.
Olson et al.
Citation for THAL SNS 032
The citations listed below are publications that use Tocris products. Selected citations for THAL SNS 032 include:
1 Citation: Showing 1 - 1
Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells
Authors: Kaji Et al.
Sci Rep 2020;10:3088
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