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Chemical Structure : THAL-SNS-032
CAS No.: 2139287-33-3
Catalog No.: PC-60330Not For Human Use, Lab Use Only.
THAL-SNS-032 is a novel CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $258 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $598 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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THAL-SNS-032 is a novel CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
THAL-SNS-032 efficiently induces complete CDK9 degradation at 250 nM (6h treatment), inhibits proliferation of MOLT4 cells at lower concentrations (IC50 = 50 nM) than SNS-032 (IC50=173 nM).
THAL-SNS-032 exhibits more potent inhibition of proliferation than SNS-032 across a panel of 11 different leukemia cancer cell lines.
THAL-SNS-032 induces rapid degradation of CDK9 without affecting the levels of other SNS-032 targets, and has prolonged cytotoxic effects.
| M.Wt | 869.022 | |
| Formula | C40H52N8O10S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
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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1. Olson CM, et al. Nat Chem Biol. 2017 Dec 18. doi: 10.1038/nchembio.2538.
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