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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.
分子量 | 326.3 |
公式 | C13H11FN2O5S |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 32.63 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: 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!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
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