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THAL SNS 032
Biological Activity for THAL SNS 032
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 Cdlk9 at 250 nM in MOLT4 cells. Inhibits proliferation of leukemia cell lines.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Sold under license from Dana-Farber Cancer Institute.
Application of THAL SNS 032 in MOLT-4 cells
Wes data showing knockdown of both CDK9 isoforms after THAL SNS 032 (Cat. No. 6532) 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 Novus NBP2-67811 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 for THAL SNS 032
|Storage||Store at -20°C|
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.
Solubility Data for THAL SNS 032
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for THAL SNS 032
The following data is based on the product molecular weight 869.02. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.75 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
References for THAL SNS 032
References are publications that support the biological activity of the product.
Olson et al (2018) Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation. Nat.Chem.Biol. 14 163 PMID: 29251720
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Keywords: THAL SNS 032, THAL SNS 032 supplier, THALSNS032, potent, selective, CDK9, active, degraders, degrades, PROTAC, PROTACs, proteolysis, targeting, chimera, targeted, protein, degradation, tpd, Active, Degraders, Transcriptional, CDKs, 6532, Tocris Bioscience
1 Citation for THAL SNS 032
Citations are publications that use Tocris products. Selected citations for THAL SNS 032 include:
Kaji et al (2020) Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells Sci Rep 10 3088 PMID: 32080280
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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