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THAL SNS 032

Catalog #: 6532
2 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
6532/5
THAL SNS 032 | CAS No. 2139287-33-3 | Cyclin-dependent Kinase Inhibitors
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Description: Potent and selective Cdk9 Degrader (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
Citations (2)
Reviews
Biological Activity Scientific Data Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

Cdk9 antibodies validated for Western Blot also available: Catalog # NBP2-15848 and NBP3-15345.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Scientific Data

Western Blot Application of THAL SNS 032 in MOLT-4 cells View Larger

Application of THAL SNS 032 in MOLT-4 cells. Western Blot data showing knockdown of both CDK9 isoforms after THAL SNS 032 treatment of MOLT-4 cells (4 h incubation). Protein quantification (relative to DMSO-only control) is shown beneath the corresponding lane. Cdk9 primary antibody is used at 1:1000 dilution. Secondary is Anti-Rabbit HAF008, 1:1000, R&D Systems. GAPDH primary antibody is R&D Systems AF5718 used at 5μg/mL. Secondary is Anti-Goat HAF017, 1:1000, R&D Systems.Data courtesy of Jeff Cooper, Bio-Techne.

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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Citations for THAL SNS 032

The citations listed below are publications that use Tocris products. Selected citations for THAL SNS 032 include:

2 Citations: Showing 1 - 2

  1. CDK9 activity is critical for maintaining MDM4 overexpression in tumor cells.
    Authors: Vladimir Et al.
    Cell Death Dis  2020;11:754
  2. Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells
    Authors: Kaji Et al.
    Sci Rep  2020;10:3088

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