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THAL-SNS-032

Chemical Structure : THAL-SNS-032

CAS No.: 2139287-33-3

THAL-SNS-032 (THAL SNS 032, CDK9 PROTAC degrader)

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).

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Biological Activity

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.

Physicochemical Properties

M.Wt 869.022
Formula C40H52N8O10S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

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

References

1. Olson CM, et al. Nat Chem Biol. 2017 Dec 18. doi: 10.1038/nchembio.2538.

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