Pricing Availability   Qty
Description: Potent covalent inhibitor of Cereblon
Chemical Name: 2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-3-oxo-1H-isoindole-5-sulfonyl fluoride
Purity: ≥95% (HPLC)
Literature (3)

Biological Activity for EM12-SO2F

EM12-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.

Technical Data for EM12-SO2F

M. Wt 326.3
Formula C13H11FN2O5S
Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 2803819-61-4
PubChem ID 165670019
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.

Solubility Data for EM12-SO2F

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 32.63 100

Preparing Stock Solutions for EM12-SO2F

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References for EM12-SO2F

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.

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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

Citations for EM12-SO2F

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Literature in this Area

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