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CRBN-6-5-5-VHL

Cat. No. 6948 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Potent and selective cereblon Degrader (PROTAC®); cell-permeable
Chemical Name: (2S,4R)-1-((2S)-2-(5-((5-((6-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)hexyl)oxy)pentyl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥96% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Scientific Data Technical Data Solubility Calculators Datasheets References

Biological Activity for CRBN-6-5-5-VHL

CRBN-6-5-5-VHL is a potent and selective cereblon Degrader (PROTAC®) (DC50 = 1.5 nM). Induces complete degradation of cereblon in MM1S cells. Comprises a cereblon E3 ligase ligand joined by a linker to a ligand for the E3 ligase VHL. Cell-permeable.

CRBN antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # NBP1-91810.

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

Scientific Data

Western Blot Application of CRBN-6-5-5-VHL in MM1S cells for CRBN-6-5-5-VHL View Larger

Application of CRBN-6-5-5-VHL in MM1S cells for CRBN-6-5-5-VHL. Western blot data showing potent knockdown of Cereblon (CRBN) mediated by the Degrader: CRBN-6-5-5-VHL in MM1S cells after 16 h incubation. IKZF1 (Ikaros) and IKZF3 (Aiolos) are transcription factors and neosubstrates of Cereblon. Application of CRBN-6-5-5-VHL does not result in degradation of these proteins. Pom; Pomalidomide. Data courtesy of Christian Steinebach, University of Bonn.

Technical Data for CRBN-6-5-5-VHL

M. Wt 972.21
Formula C51H69N7O10S
Storage Store at -20°C
Purity ≥96% (HPLC)
CAS Number 2362575-45-7
Smiles CC1=C(SC=N1)C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@@H](NC(CCCCOCCCCCOCCCCCCNC4=CC=CC(C(N5C6CCC(NC6=O)=O)=O)=C4C5=O)=O)C(C)(C)C)=O)=O)C=C2

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 CRBN-6-5-5-VHL

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 97.22 100

Preparing Stock Solutions for CRBN-6-5-5-VHL

The following data is based on the product molecular weight 972.21. 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 1.03 mL 5.14 mL 10.29 mL
5 mM 0.21 mL 1.03 mL 2.06 mL
10 mM 0.1 mL 0.51 mL 1.03 mL
50 mM 0.02 mL 0.1 mL 0.21 mL

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Product Datasheets for CRBN-6-5-5-VHL

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for CRBN-6-5-5-VHL

References are publications that support the biological activity of the product.

Steinebach et al (2019) PROTAC-mediated crosstalk between E3 ligases. Chem.Commun.(Camb) 55 1821 PMID: 30672516

If you know of a relevant reference for CRBN-6-5-5-VHL, please let us know.

View Related Products by Target

Keywords: CRBN-6-5-5-VHL, CRBN-6-5-5-VHL supplier, PROTACs, proteolysis, targeting, chimeras, active, Degraders, degrades, VHL, von, Hippel, Lindau, Cereblon, CRBN, PROTAC, targeted, protein, degradation, tpd, Ubiquitin, E3, Ligases, Ligase, 6948, Tocris Bioscience

Citations for CRBN-6-5-5-VHL

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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
  • Induced Proximity Tools
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