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Submit ReviewJNJ 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.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 87.81 | 100 |
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.
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 |
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, IRAK, Kinase, 8029, Tocris Bioscience
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This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
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