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C188-9 is a small-molecule STAT3 inhibitor, can block Th2 and Th17 cell expansion and cytokine production to prevent house dust mite (HDM)-induced airway inflammation and remodeling. C188-9 showed antitumor activity in vitro in three hepatocellular carcinoma cell lines.
In mice with hepatocyte-specific deletion of Pten (HepPten- mice), C188-9 treatment blocked hepatocellular carcinoma tumor growth, reduced tumor development, and reduced liver steatosis, inflammation, and bile ductular reactions, resulting in improvement of the pathological lesions of NASH. Remarkably, C188-9 also greatly reduced liver injury in these mice as measured by serum aspartate aminotransferase and alanine transaminase levels.
Analysis of gene expression showed that C188-9 treatment of HepPten- mice resulted in inhibition of signaling pathways downstream of STAT3, STAT1, TREM-1, and Toll-like receptors. In contrast, C188-9 treatment increased liver specification and differentiation gene pathways.
| Molecular Weight | 471.52 |
| Formula | C27H21NO5S |
| CAS Number | 432001-19-9 |
| Solubility (25°C) | DMSO ≥ 40 mg/mL |
| Storage | 2-8°C, dry, protect from light, sealed |
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