IRAK3 Degrader 23

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Description: IRAK3 Degrader (PROTAC®
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)
Datasheet
Citations
Reviews
Literature (2)

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
InChI Key ZUODKONSNNHSAJ-AMLBMYBGSA-N
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
Solubility
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.

View Related Products by Target

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Citations for IRAK3 Degrader 23

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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

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

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

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