A small molecule inhibitor of NF-κB-dependent expression of TNF-α

Ro 106-9920 – 10 mg

Brand:
Cayman
CAS:
62645-28-7
Storage:
-20
UN-No:
Non-Hazardous - /

Transcriptional activation by NF-κB is limited by IκBα binding, which masks the NF-κB nuclear localization signal that initiates nuclear translocation. Cytokines trigger a signaling cascade of kinases that target IκBα for degradation, enabling NF-κB to promote gene expression. Because NF-κB regulates the transcription of inflammatory mediators, blocking its signaling activity is regarded as an effective means to treat inflammatory diseases. Ro 106-9920 is a small molecule inhibitor of NF-κB-dependent expression of TNF-α, interleukin-1β, and interleukin-6 (IC50 50 value of 2.3 µM demonstrating little activity against the ubiquitin-activating enzyme E1 (IC50s >100 µM), the ubiquinating-conjugating enzyme E2UBCH7, nonspecific ubiquitination of cellular proteins, and 97 other molecular targets.{25615} In two different models of acute inflammation, Ro 106-9920 at 10-100 mg/kg has been shown to dose-dependently inhibit cytokine production in rat.{25615}  

 

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Description

A small molecule inhibitor of NF-κB-dependent expression of TNF-α, IL-1β, and IL-6 (IC50 50 = 2.3 µM)

Formal name: 6-(phenylsulfinyl)-tetrazolo[1,5-b]pyridazine

Synonyms: 

Molecular weight: 245.3

CAS: 62645-28-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|TNF-α/NF-κB Signaling||Research Area|Cell Biology|Cell Signaling|NF-κB Signaling||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Immunology & Inflammation|Innate Immunity

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