(E)-SIS3 is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation. (E)-SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.
IC50&Target
IC50: 3 μM (Smad3 phosphorylation)
体外研究
(E)-SIS3 (0.3-10 μM; for 1 hour) attenuates the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4.
(E)-SIS3 (0.1 , 10, 50 μM; 30 min) significantly suppresses the expression of FN and α-SMA, but not that of Sphk2 provoked by TGF-β1.
(E)-SIS3 (10 μM; 24 hours) significantly reduces both α-SMA and palladin expression that is enhanced by TWEAK in Primary human dermal fibroblasts.
(E)-SIS3 significantly inhibits L4 development at five concentrations from as low as 2 µM to 50 µM (5 µM, 10 µM, 20 µM and 50 µM) in a dose-dependent manner.
Western Blot Analysis
Cell Line:
Human dermal fibroblasts
Concentration:
0.3, 1, 3, 10 μM
Incubation Time:
For 1 hour
Result:
Attenuated the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4.
分子式
C28H27N3O3.HCl
分子量
489.99
CAS号
521984-48-5
中文名称
SIS3 盐酸盐
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 125 mg/mL (255.11 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)