THAL SNS 032

Catalog # Availability Size / Price Qty
6532/5
Cat.No. 6532 - THAL SNS 032 | C40H52N8O10S2 | CAS No. 2139287-33-3
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Description: Potent and selective CDK9 degrading PROTAC

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

Purity: ≥98%

Product Details
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Biological Activity

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.

Technical Data

M.Wt:
869.02
Formula:
C40H52N8O10S2
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2139287-33-3

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.

Additional Information

Licensing Caveats:
Sold under license from Dana-Farber Cancer Institute.

Background References

  1. Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation.
    Olson et al.
    Nat.Chem.Biol., 2018;14:163

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