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SIS3 is a novel specific inhibitor of TGF-β1/ALK-5 phosphorylation of Smad3. SIS3 inhibits Smad3 phosphorylation with an IC50 of 3 µM. SIS3 inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways.
SIS3 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.
| 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 |
| Related TGF-beta/Smad Products |
|---|
| A 83-01 sodium
A 83-01 sodium is a potent inhibitor of TGF-β type I receptors ALK5, ALK4, and ALK7, inhibiting ALK5, ALK4, and ALK7-induced transcription with IC50 values of 12 nM, 45 nM, and 7.5 nM, respectively. |
| Myristoyl tetrapeptide-12
Myristoyl tetrapeptide-12 directly activates SMAD2 and induces the linking of SMAD3 with DNA. |
| H-Leu-Ser-Lys-Leu-OH
H-Leu-Ser-Lys-Leu-OH (LSYL) is a latency-associated peptide at the amino terminus of LAP, with inhibitory effect on TGF-β1 activation. |
| SY-LB-35
SY-LB-35 is a potent bone morphogenetic protein (BMP) receptor agonist. |
| DT-6
DT-6 is an effective TGF-β1 inhibitor. |
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