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A cell permeable imidazoxanthine shown to decrease TGF-β stimulated reporter activity in a dose-dependent manner in HEK293 reporter cells, with an IC50 of 4.1 µM without cell cytotoxicity. Inhibits TGF-β receptor I (TβRI) and TGF-β receptor II (TβRII) expression and its downstream Smad2 and Smad3 phosphorylation as well as JNK and ERK activity. In addition, it elicits TGF-β-induced fibroblast differentiation with attenuated expression of several fibrotic markers such as α-SMA and fibronectin, and suppresses collagen accumulation in CCD-18Lu human normal lung fibroblasts.
Park, S., et al. 2010. Biochem. Biophy. Res. Comm.399, 268.
数据表
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A cell permeable imidazoxanthine shown to decrease TGF-β stimulated reporter activity in a dose-dependent manner in HEK293 reporter cells, with an IC50 of 4.1 µM without cell cytotoxicity. Inhibits TGF-β receptor I (TβRI) and TGF-β receptor II (TβRII) expression and its downstream Smad2 and Smad3 phosphorylation as well as JNK and ERK activity. In addition, it elicits TGF-β-induced fibroblast differentiation with attenuated expression of several fibrotic markers such as α-SMA and fibronectin, and suppresses collagen accumulation in CCD-18Lu human normal lung fibroblasts.
Form
Off-white solid
Chemical formula
C₁₆H₁₄ClN₅O₂
Structure formula
Purity
≥90% by HPLC
Solubility
DMSO (3 mg/ml)
Storage
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Park, S., et al. 2010. Biochem. Biophy. Res. Comm.399, 268.
