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Submit ReviewEM 163 is a TIR-TIR interaction inhibitor, that is a TIR (Toll/ interleukin-1 receptor) domain peptidomimetic of MyD88 protein. EM 163 targets TIR domains in IL-1 receptors blocking the interaction with MyD88. EM 163 inhibits staphylococcal enterotoxin B (SEB)-induced inflammatory cytokine production in vivo. EM 163 protects mice from SEB shock-induced death. In rat hippocampal neurons in vitro, EM 163 blocks the activation of p38 and the inhibitory effects of IL-1β on protein synthesis triggered by chemically-induced long-term potentiation (LTP).
M. Wt | 849.9 |
Formula | C44H60IN5O4 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 1206480-93-4 |
PubChem ID | 44602511 |
InChI Key | WJCJDZIXEVJIKZ-OFUZFLEOSA-M |
Smiles | CC([C@@H](C(N1CCCC1)=O)N(C(C2=C[N+](C)=C(C(N([C@H](C(N3CCCC3)=O)C(C)C)CCCC4=CC=CC=C4)=O)C=C2)=O)CCCC5=CC=CC=C5)C.[I-] |
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 | 84.99 | 100 |
The following data is based on the product molecular weight 849.9. 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 | 1.18 mL | 5.88 mL | 11.77 mL |
5 mM | 0.24 mL | 1.18 mL | 2.35 mL |
10 mM | 0.12 mL | 0.59 mL | 1.18 mL |
50 mM | 0.02 mL | 0.12 mL | 0.24 mL |
References are publications that support the biological activity of the product.
Prieto et al (2019) Inhibition of LTP-induced translation by IL-1β reduces the level of newly synthesized proteins in hippocampal dendrites. ACS Chem.Neurosci. 20 1197 PMID: 30695637
Kissner et al (2012) Therapeutic inhibition of pro-inflammatory signaling and toxicity to staphylococcal enterotoxin B by a synthetic dimeric BB-loop mimetic of MyD88. PLoS One 7 e40773 PMID: 22848400
Lucas and Maes (2013) Role of the toll like receptor (TLR) radical cycle in chronic inflammation: possible treatments targeting the TLR4 pathway. Mol.Neurobiol. 48 190 PMID: 23436141
If you know of a relevant reference for EM 163, please let us know.
Keywords: EM 163, EM 163 supplier, EM163, inhibitors, inhibits, Cytokines, cytokines, MyD88, anti-inflammatory, interleukin-1, TIR, IL-1, Cytokine, Receptors, 7010, Tocris Bioscience
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