Ro 106-9920

Transcriptional activation by NF-kappaB is limited by IkappaBalpha binding, which masks the NF-kappaB nuclear localization signal that initiates nuclear translocation. Cytokines trigger a signaling cascade of kinases that target IkappaBalpha for degradation, enabling NF-kappaB to promote gene expression. Because NF-kappaB 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-kappaB-dependent expression of TNF-alpha, interleukin-1beta, 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. 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.Formal Name: 6-(phenylsulfinyl)-tetrazolo[1,5-b]pyridazine. CAS Number: 62645-28-7. Molecular Formula: C10H7N5OS. Formula Weight: 245.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 20 mg/ml. lambdamax: 205, 231 nm. SMILES: O=S(C(C=C1)=NN2C1=NN=N2)C3=CC=CC=C3. InChi Code: InChI=1S/C10H7N5OS/c16-17(8-4-2-1-3-5-8)10-7-6-9-11-13-14-15(9)12-10/h1-7H. InChi Key: JFSXSNSCPNFCDM-UHFFFAOYSA-N.