THAL SNS 032

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Cat.No. 6532 - THAL SNS 032 | C40H52N8O10S2 | CAS No. 2139287-33-3
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% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

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 Cdlk9 at 250 nM in MOLT4 cells. Inhibits proliferation of leukemia cell lines.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Application of THAL SNS 032 in MOLT-4 cells

Application of THAL SNS 032 in MOLT-4 cells (Cat. No. 6532)



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.

Data courtesy of Jeff Cooper, Bio-Techne.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 86.9 100

Preparing Stock Solutions

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

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References

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.

Keywords: THAL SNS 032, THAL SNS 032 supplier, THALSNS032, potent, selective, CDK9, degraders, degrades, PROTAC, proteolysis, targeting, chimera, Active, Degraders, Cyclin-dependent, Kinase, 6532, Tocris Bioscience

Citations for THAL SNS 032

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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* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Targeted Protein Degradation

Targeted Protein Degradation Research Product Guide

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

  • Active Degraders (e.g. PROTACs)
  • Degrader Building Blocks
  • Custom Degrader Services
  • UPS Proteins and Assays
  • Assays for Protein Degradation
Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics in Cancer

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Targeted Protein Degradation

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