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Submit ReviewHDAC4 CHDI Degrader 11
Description: Potent and selective HDAC4 Degrader (PROTAC®)
Chemical Name: (2S,4R)-1-((3R,26S)-26-(tert-Butyl)-3-methyl-1,24-dioxo-5-propyl-1-(4-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)phenyl)-10,13,16,19,22-pentaoxa-2,5,25-triazaheptacosan-27-oyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Biological Activity for HDAC4 CHDI Degrader 11
HDAC4 CHDI Degrader 11 is a potent and selective HDAC4 Degrader (PROTAC®) (DC50 values are 4 and 6 nM in Jurkat E6-1 and Jurkat cells respectively). Comprises the class IIa HDAC inhibitor trifluoromethyloxadiazole joined by a linker to a ligand for Von Hippel-Lindau (VHL) protein. In a mouse cell model of Huntington's disease, HDAC4 CHDI Degrader 11 potently degrades HDAC4 (DC50 = 1nM). Can be used with P-glycoprotein inhibitor Elacridar (Cat. No. 4646) for more effective degradation in neuroblastoma cell lines.
HDAC4 antibody validated for Simple Western™ (automated Western) instruments also available: Catalog # NBP2-22151.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Technical Data for HDAC4 CHDI Degrader 11
| M. Wt | 1075.26 |
| Formula | C52H73F3N8O11S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 3035189-46-6 |
| InChI Key | KBDZFZJFGKYVBZ-KLSSUPLUSA-N |
| Smiles | O=C(NCC1=CC=C(C=C1)C2=C(N=CS2)C)[C@H]3N(C[C@@H](C3)O)C([C@@H](NC(COCCOCCOCCOCCOCCCCN(C[C@H](NC(C4=CC=C(C=C4)C5=NOC(C(F)(F)F)=N5)=O)C)CCC)=O)C(C)(C)C)=O |
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 HDAC4 CHDI Degrader 11
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 53.76 | 50 |
Preparing Stock Solutions for HDAC4 CHDI Degrader 11
The following data is based on the product molecular weight 1075.26. 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 |
|---|---|---|---|
| 0.5 mM | 1.86 mL | 9.3 mL | 18.6 mL |
| 2.5 mM | 0.37 mL | 1.86 mL | 3.72 mL |
| 5 mM | 0.19 mL | 0.93 mL | 1.86 mL |
| 25 mM | 0.04 mL | 0.19 mL | 0.37 mL |
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Product Datasheets for HDAC4 CHDI Degrader 11
References for HDAC4 CHDI Degrader 11
References are publications that support the biological activity of the product.
Macabuag et al (2022) Developing HDAC4-selective protein degraders to investigate the role of HDAC4 in Huntington's disease pathology. J.Med.Chem. 6512445 PMID: 36098485
If you know of a relevant reference for HDAC4 CHDI Degrader 11, please let us know.
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Citations for HDAC4 CHDI Degrader 11
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Epigenetics in Cancer Research Product Guide
This product guide reviews some of the main areas in cancer epigenetics research and lists around 120 products that can be used for the main epigenetic targets including:
- Histone Methylation
- Histone Acetylation
- DNA Methylation
- Ubiquitination
- Bromodomains
TPD and Induced Proximity Research Product GuideUpdated
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
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