JNJ 1013

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Description: Interleukin 1 Receptor Associated Kinase 1 (IRAK1) Degrader (PROTAC®)
Chemical Name: N-(4-(4-(2-(((S)-1-((2S,4R)-4-Hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)piperidin-1-yl)-2-methoxyphenyl)-6-(1H-pyrazol-5-yl)picolinamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity for JNJ 1013

JNJ 1013 is a potent interleukin 1 receptor associated kinase 1 (IRAK1) Degrader (PROTAC®; DC50 = 3 nM; Dmax = 96%). In ABC DLBCL cell lines with MyD88 L265P mutation, JNJ 1013 potently inhibits IRAK1 downstream signaling pathways, induces apoptosis, and shows strong anti-proliferative effects.

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

Technical Data for JNJ 1013

M. Wt 878.06
Formula C46H55N9O7S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2597343-08-1
PubChem ID 162660665
InChI Key MHRNVFQJUUXQIG-VIFUUBRESA-N
Smiles COC(C=C1N(CC2)CCC2OCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@H](C3)O)C(N[C@H](C4=CC=C(C5=C(C)N=CS5)C=C4)C)=O)=O)=O)=C(C=C1)NC(C6=CC=CC(C7=NNC=C7)=N6)=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 JNJ 1013

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

Preparing Stock Solutions for JNJ 1013

The following data is based on the product molecular weight 878.06. 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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References for JNJ 1013

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

Fu et al (2021) Discovery of highly potent and selective IRAK1 Degraders to probe scaffolding functions of IRAK1 in ABC DLBCL. J.Med.Chem. 64 10878 PMID: 34279092


If you know of a relevant reference for JNJ 1013, please let us know.

Keywords: JNJ 1013, JNJ 1013 supplier, JNJ1013, interleukin1, receptor, associated, kinase, 1, active, degraders, degrades, selective, protac, PROTACs, proteolysis, targeting, chimera, Degraders, apoptosis, cell, survival, Protein, IRAK, 8029, Tocris Bioscience

Citations for JNJ 1013

Citations are publications that use Tocris products.

Currently there are no citations for JNJ 1013. Do you know of a great paper that uses JNJ 1013 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!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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