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THAL SNS 032

Cat. No. 6532 2 Citations Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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% (HPLC)
Datasheet
Citations (2)
Reviews
Literature (2)
Biological Activity Scientific Data Technical Data Solubility Calculators Datasheets References

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 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.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Technical Data for THAL SNS 032

M. Wt 869.02
Formula C40H52N8O10S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2139287-33-3
PubChem ID 131801483
InChI Key BXDZOYLPNAIDOC-UHFFFAOYSA-N
Smiles CC(C)(C1=CN=C(O1)CSC2=CN=C(S2)NC(C3CCN(CC3)CC(NCCOCCOCCOCCNC4=C5C(N(C(C5=CC=C4)=O)C6CCC(NC6=O)=O)=O)=O)=O)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
Solubility
DMSO 86.9 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for THAL SNS 032

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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

If you know of a relevant reference for THAL SNS 032, please let us know.

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2 Citations for THAL SNS 032

Citations are publications that use Tocris products. Selected citations for THAL SNS 032 include:

Vladimir et al (2020) CDK9 activity is critical for maintaining MDM4 overexpression in tumor cells. Cell Death Dis 11 754 PMID: 32934219

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

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
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Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia