99840-40-1

Upstream product

• 100-02-7 4-nitro-phenol 
• 628-77-3 1,5-diiodopentane 

Downstream Products

• 101939-29-1 3-[5-(4-nitro-phenoxy)-pentyl]-thiazolidine-2,4-dione 
• 109444-74-8 trimethyl-[5-(4-nitro-phenoxy)-pentyl]-ammonium; iodide 
• 101438-70-4 1-[5-(4-amino-phenoxy)-pentyl]-piperidin-2-one 
• 101586-61-2 1-[5-(4-amino-phenoxy)-pentyl]-1H-pyridin-2-one 
• 106273-32-9 3-[5-(4-amino-phenoxy)-pentyl]-thiazolidine-2,4-dione 
• 93429-13-1 4-(3-(4-nitrophenoxy)propyl)morpholine 
• 1394355-86-2 C₁₆H₂₀N₂O₃S₂ 
• 1394355-99-7 C₃₀H₂₉N₃O₅S₂ 
• 1394356-00-3 C₃₀H₂₉N₃O₅S₂ 
• 1394356-01-4 C₃₀H₂₉N₃O₅S₂ 
• 1394356-02-5 C₂₈H₂₇N₃O₅S₂ 
• 1394356-03-6 C₂₈H₂₇N₃O₅S₂ 
• 100800-40-6 4-[3-(morpholin-4-yl)propoxy]aniline 
• 101586-59-8 4-(5-[2]pyridyloxy-pentyloxy)-aniline 

Relevant academic research and scientific papers

Discovery of potent and selective rhodanine type IKKβ inhibitors by hit-to-lead strategy

Regulation of NF-κB activation through the inhibition of IKKβ has been identified as a promising target for the treatment of inflammatory and autoimmune disease such as rheumatoid arthritis. In order to develop novel IKKβ inhibitors, we performed high throughput screening toward around 8000 library compounds, and identified a hit compound containing rhodanine moiety. We modified the structure of hit compound to obtain potent and selective IKKβ inhibitors. Throughout hit-to-lead studies, we have discovered optimized compounds which possess blocking effect toward NF-κB activation and TNFα production in cell as well as inhibition activity against IKKβ. Among them, compound 3q showed the potent inhibitory activity against IKKβ, and excellent selectivity over other kinases such as p38α, p38β, JNK1, JNK2, and JNK3 as well as IKKα.