WDR5 PROTAC® Homer New
Tocris Bioscience, part of Bio-Techne | Catalog # 7986
Potent and selective WDR5 PROTAC® Degrader
Key Product Details
Description
Potent and selective WDR5 PROTAC® Degrader
Product Description
WDR5 PROTAC® Homer is a potent and selective WD-repeat-containing protein 5 (WDR5) Degrader (KD (ITC) = 18 nM). Comprises the WDR5-binding probe OICR 9429 (Cat. No. 5267), joined by a linker to a Von Hippel-Lindau (VHL) E3 ubiquitin ligase-recruiting ligand. Displays cellular activity in MV4-11 cells (DC50 = 53 nM; DCmax = 58%) by inducing degradation of WDR5 in a catalytic manner. Displays selectivity for WDR5 over 5805 proteins detected in quantitative proteomics experiments performed in MV4-11 cells.PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the Homer probe summary on the SGC website.External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of Homer is reviewed on the chemical probes website.Product Specifications
Molecular Weight
1012.16
Formula
C52H60F3N9O7S
Storage
Store at -20°C
Purity
≥95% (HPLC)
Chemical Name
N-(4'-((5-(((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-5-oxopentyl)carbamoyl)-4-(4-methylpiperazin-1-yl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
CAS Number
2737222-94-3
PubChem ID
157049306
InChI Key
OFNZESNEBSQKSE-BQGOKDIQSA-N
SMILES
O=C(C(C(C(F)(F)F)=C1)=CNC1=O)NC2=C(N3CCN(CC3)C)C=CC(C4=CC=C(C=C4)C(NCCCCC(N[C@@H](C(C)(C)C)C(N5[C@@H](C[C@H](C5)O)C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)=O)=C2
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 10.12 | 10 |
Preparing Stock Solutions
for WDR5 PROTAC® Homer
The following data is based on the product molecular weight 1012.16
Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 9.88 mL | 49.40 mL | 98.80 mL |
| 0.5 mM | 1.98 mL | 9.88 mL | 19.76 mL |
| 1 mM | 0.99 mL | 4.94 mL | 9.88 mL |
| 5 mM | 0.20 mL | 0.99 mL | 1.98 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Dölle Design, synthesis, and evaluation of WD-repeat-containing protein 5 (WDR5) degraders. J.Med.Chem. 2021 PMID: 33980013
Product Specific Notices for WDR5 PROTAC® Homer
For research use only
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