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SIS3 hydrochloride is a novel specific inhibitor of TGF-β1/ALK-5 phosphorylation of Smad3. SIS3 hydrochloride inhibits Smad3 phosphorylation with an IC50 of 3 µM. SIS3 hydrochloride inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways.
SIS3 hydrochloride significantly reduces collagen IV and fibronectin expression in the glomeruli and tubulointerstitium of STZ-injected Tie2-Cre;Loxp-EGFP mice, suggesting that SIS3 retards the early development of STZ-induced diabetic glomerulosclerosis and tubulointerstitial fibrosis. However, SIS3 administration does not reduce proteinuria.
Cytokine. 2026 Jan 10;199:157113.
IL-6 trans-signaling activates the TGF-β pathway via soluble factors in difficult-to-treat rheumatoid arthritis joint fluid
SIS3 hydrochloride purchased from AbMole
| Molecular Weight | 489.99 |
| Formula | C28H27N3O3.HCl |
| CAS Number | 521984-48-5 |
| Solubility (25°C) | DMSO: ≥ 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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