| Identification | Back Directory | [Name]
SR12343 | [CAS]
2055101-86-3 | [Synonyms]
SR12343
Acetamide, N-[2-(3-bromophenyl)ethyl]-2-[(5-chloro-2-pyridinyl)amino]- | [Molecular Formula]
C15H15BrClN3O | [MOL File]
2055101-86-3.mol | [Molecular Weight]
368.66 |
| Chemical Properties | Back Directory | [Boiling point ]
603.4±55.0 °C(Predicted) | [density ]
1.496±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml | [form ]
A crystalline solid | [pka]
14.86±0.46(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
SR12343, an IKK/NF-κB inhibitor, is a NF-κB essential modulator (NEMO)-binding domain (NBD) mimetic. SR12343 inhibits TNF-α- and LPS-induced NF-κB activation by blocking the interaction between IKKβ and NEMO, with an IC50 of 37.02 μM for TNF-α-mediated NF-κB activation. SR12343 suppresses LPS-induced acute pulmonary inflammation in mice. SR12343 can be used for research of inflammatory and degenerative diseases[1]. | [Biological Activity]
SR 12343 is a mimetic of the IκB kinase β (IKKβ) NEMO/IKKγ-binding domain (NBD) that inhibits the protein-protein interaction between the IKK complex subunits NF-κB essential modulator (NEMO/IKKγ) and IKKβ.1 It selectively disrupts the association of NEMO/IKKγ with IKKβ over TNF receptor-associated factor 2 (TRAF2), IκBα, and IKKα in co-immunoprecipitation assays using RAW 264.7 cells at concentrations ranging from 25 to 150 μM. SR 12343 inhibits TNF-α-induced NF-κB activation in a reporter assay. It reduces increased serum IL-6 levels in a mouse model of LPS-induced endotoxemia when administered at a dose of 10 mg/kg. SR 12343 (30 mg/kg) improves grip strength and reduces muscle fibrosis in the mdx mouse model of Duchenne muscular dystrophy. | [References]
1.Zhao, J., Zhang, L., Mu, X., et al.Development of novel NEMO-binding domain mimetics for inhibiting IKK/NF-kB activationPLoS Biol.16(6)e2004663(2018)
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| Company Name: |
ChemeGen
|
| Tel: |
18818260767 |
| Website: |
https://www.chemegen.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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