HDAC4 CHDI Degrader 11

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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)
Datasheet
Citations
Reviews
Literature (4)

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)
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.

Select a batch to recalculate based on the batch molecular weight:
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.

Keywords: HDAC4 CHDI Degrader 11, HDAC4 CHDI Degrader 11 supplier, HDAC4CHDIDegrader11, protac, degrader, degraders, degrades, potent, selective, VHL, von, hippel, lindau, huntingtons, huntingtin, HDAC4, HDAC, neurodegeneration, Protein, Degraders, Class, II, HDACs, 7882, Tocris Bioscience

Citations for HDAC4 CHDI Degrader 11

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Literature in this Area

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Targeted Protein Degradation Research Product Guide

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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.

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Targeted Protein Degradation Poster

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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