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 Cdlk9 at 250 nM in MOLT4 cells. Inhibits proliferation of leukemia cell lines.
THAL 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.
Caractéristiques techniques
| Marque | Tocris Bioscience |
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| Réf. B-LABO | BL-RE-124973 |
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| Réf. fabricant | 18729286 |
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| Nom chimique ou matériau | 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 |
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| CAS | 2139287-33-3 |
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| Quantité | 5 mg |
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| Formule moléculaire | C<sub>40</sub>H<sub>52</sub>N<sub>8</sub>O<sub>10</sub>S<sub>2</sub> |
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| Poids de la formule | 869.02 |
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| Pureté | 98% |
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