SJ 10542

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Description: Potent and selective JAK2/3 Degrader (PROTAC®)
Chemical Name: 4-((4-(1-(3-(Cyanomethyl)-1-(ethylsulfonyl)azetidin-3-yl)-1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-N-(3-(4-(4-(2,6-dioxopiperidin-3-yl)phenyl)piperazin-1-yl)propyl)benzamide
Purity: ≥97% (HPLC)
Datasheet
Citations
Reviews
Literature (4)

Biological Activity for SJ 10542

SJ 10542 is a potent and selective JAK2/3 Degrader (PROTAC®) (DC50 values are 11 nM and 14 nM for JAK3 and JAK2, respectively), it uses a phenyl glutarimide (PG) ligand as the cereblon (CRBN) recruiter. SJ 10542 displays high selectivity over GSPT1 and other members of the JAK family. SJ 10542 is active in cytotoxicity assays with PDX models (IC50 values <120 nM).

JAK3 antibody validated for Western Blot also available: Catalog # MAB4699.

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

Licensing Information

Sold under license from St. Jude Children's Research Hospital

Technical Data for SJ 10542

M. Wt 818.96
Formula C41H46N12O5S
Storage Store at -20°C
Purity ≥97% (HPLC)
CAS Number 2789678-92-6
PubChem ID 162679331
InChI Key WBEBZVDAHMXWJN-UHFFFAOYSA-N
Smiles O=C(NC1=O)CCC1C2=CC=C(N3CCN(CCCNC(C4=CC=C(NC5=NC6=C(C=CN6)C(C7=CN(C8(CC#N)CN(S(CC)(=O)=O)C8)N=C7)=N5)C=C4)=O)CC3)C=C2

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 SJ 10542

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 40.95 50

Preparing Stock Solutions for SJ 10542

The following data is based on the product molecular weight 818.96. 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 2.44 mL 12.21 mL 24.42 mL
2.5 mM 0.49 mL 2.44 mL 4.88 mL
5 mM 0.24 mL 1.22 mL 2.44 mL
25 mM 0.05 mL 0.24 mL 0.49 mL

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References for SJ 10542

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

Alcock et al (2022) Development of potent and selective Janus Kinase 2/3 directing PG-PROTACs. ACS Med.Chem.Lett. 13 475 PMID: 35300081


If you know of a relevant reference for SJ 10542, please let us know.

Keywords: SJ 10542, SJ 10542 supplier, SJ10542, protacs, active, degraders, selective, JAK3, JAK2, kinases, degrades, proteolysis, targeting, chimeras, PROTAC, PROTACS, targeted, protein, degradation, tpd, baricitinib, Protein, Degraders, JAK, 7727, Tocris Bioscience

Citations for SJ 10542

Citations are publications that use Tocris products.

Currently there are no citations for SJ 10542. Do you know of a great paper that uses SJ 10542 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