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Submit ReviewEM12-SO2F is a potent covalent Cereblon (CRBN) inhibitor (IC50 = 0.88 nM). Binds to a histidine residue (His353) in the IMiD binding pocket of CRBN and blocks the recruitment of its substrates. EM12-SO2F prevents Lenalidomide (Cat. No. 6305)-induced degradation of the zinc finger transcription factor IKZF1 in MOLT4 cells. It complements CRBN based PROTAC and genetic methods to validate CRBN-mediated degradation.
M. Wt | 326.3 |
Formula | C13H11FN2O5S |
Storage | Store at -20°C |
Purity | ≥95% (HPLC) |
CAS Number | 2803819-61-4 |
PubChem ID | 165670019 |
InChI Key | IAJNULNMWPZFDR-UHFFFAOYSA-N |
Smiles | O=C1NC(C(CC1)N2C(C3=CC(S(=O)(F)=O)=CC=C3C2)=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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 32.63 | 100 |
The following data is based on the product molecular weight 326.3. 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 | 3.06 mL | 15.32 mL | 30.65 mL |
5 mM | 0.61 mL | 3.06 mL | 6.13 mL |
10 mM | 0.31 mL | 1.53 mL | 3.06 mL |
50 mM | 0.06 mL | 0.31 mL | 0.61 mL |
References are publications that support the biological activity of the product.
Cruite et al (2022) Cereblon covalent modulation through structure-based design of histidine targeting chemical probes. RSC Chem.Biol. 3 1105 PMID: 36128501
If you know of a relevant reference for EM12-SO2F, please let us know.
Keywords: EM12-SO2F, EM12-SO2F supplier, EM12SO2F, inhibitor, inhibitors, inhibit, inhibits, Cereblon, CRBN, His353, PROTAC, Targeted, protein, degradation, TPD, Ubiquitin, E3, Ligases, 7852, Tocris Bioscience
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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.
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.
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