CRBN-6-5-5-VHL

Name: CRBN-6-5-5-VHL
Brand: Tocris Bioscience
SKU: 6948

Tocris Bioscience, part of Bio-Techne | Catalog # 6948

COA / SDS

Potent and selective cereblon Degrader (PROTAC®); cell-permeable

Key Product Details

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)
Molecular Weight:	972.21

View Full Technical Details for CRBN-6-5-5-VHL

Technical Data
Citations

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 Examples for CRBN-6-5-5-VHL

	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 for CRBN-6-5-5-VHL

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

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	0.10 mL	0.51 mL	1.03 mL
50 mM	0.02 mL	0.10 mL	0.21 mL

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References for CRBN-6-5-5-VHL

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

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