THAL-SNS-032 is a selective CDK9 degrader. THAL-SNS-032 consists of a CDK-binding SNS-032 ligand linked to a thalidomide.
CAS Number: 2139287-33-3
Molecular Weight: 869.02
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
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 100 mg/mL(115.07 mM). Water: Insoluble.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
THAL-SNS-032 is a selective CDK9 degrader consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative which binds the E3 ubiquitin ligase Cereblon (CRBN). THAL-SNS-032 induces rapid degradation of CDK9 without affecting the levels of other SNS-032 targets. The transcriptional changes elicited by THAL-SNS-032 are more like those caused by NVP-2 than those induced by SNS-032. Strikingly, compound washout does not significantly reduce levels of THAL-SNS-032-induced apoptosis, suggesting that CDK9 degradation had prolonged cytotoxic effects compared to CDK9 inhibition.
- Calla M Olson, et al. Nat Chem Biol. 2018 Feb;14(2):163-170.
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