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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)
Literature (4)

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

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
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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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.

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, Protein, Ubiquitin, E3, Ligases, 6948, Tocris Bioscience

Citations for CRBN-6-5-5-VHL

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Literature in this Area

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Targeted Protein Degradation Research Product Guide

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
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Ubiquitin-Proteasome System Proteins
  • Assays for Protein Degradation
Epigenetics Scientific Review

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 Poster

Epigenetics in Cancer Poster

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 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