IRAK3 Degrader 23

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Description: IRAK3 PROTAC® Degrader
Chemical Name: 2-(2,6-Dioxo-3-piperidyl)-5-[4-[2-[1-[4-[4-[cis-4-[(5-isopropylpyrrolo[2,1-f][1,2,4]triazin-4-yl)amino]cyclohexyl]-piperazin-1-yl]-4-oxo-butanoyl]-4-piperidyl]ethyl]piperazin-1-yl]-isoindoline-1,3-dione
Purity: ≥98% (HPLC)
Literature (4)

Biological Activity for IRAK3 Degrader 23

IRAK3 Degrader 23 is a potent and selective IRAK3 Degrader (PROTAC®; DC50 = 2 nM; Dmax = 98% in THP1 cells and primary macrophages), requires CRBN and IRAK3 binding for Degrader activity. Also inhibits CDK11, CDK8, TRKC and GSG2 (IC50 values are 16 nM, 36 nM, 100 nM and 110 nM respectively).

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Technical Data for IRAK3 Degrader 23

M. Wt 878.09
Formula C47H63N11O6
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2712600-00-3
PubChem ID 162366970
Smiles O=C1C2=CC(N3CCN(CC3)CCC4CCN(CC4)C(CCC(N5CCN([C@@H]6CC[C@@H](CC6)NC7=NC=NN8C7=C(C(C)C)C=C8)CC5)=O)=O)=CC=C2C(N1C9C(NC(CC9)=O)=O)=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 IRAK3 Degrader 23

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 87.81 100

Preparing Stock Solutions for IRAK3 Degrader 23

The following data is based on the product molecular weight 878.09. 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 1.14 mL 5.69 mL 11.39 mL
5 mM 0.23 mL 1.14 mL 2.28 mL
10 mM 0.11 mL 0.57 mL 1.14 mL
50 mM 0.02 mL 0.11 mL 0.23 mL

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Product Datasheets for IRAK3 Degrader 23

References for IRAK3 Degrader 23

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

Degorce et al (2020) Discovery of proteolysis-targeting chimera molecules that selectively degrade the IRAK3 pseudokinase. J.Med.Chem. 63 10460 PMID: 32803978

If you know of a relevant reference for IRAK3 Degrader 23, please let us know.

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Citations for IRAK3 Degrader 23

Citations are publications that use Tocris products.

Currently there are no citations for IRAK3 Degrader 23. Do you know of a great paper that uses IRAK3 Degrader 23 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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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