SIS3

Research use only, not for human use.

Selective Smad3 inhibitor; attenuates TGF-β1-dependent Smad3 phosphorylation and Dna binding.

Selective Smad3 inhibitor; attenuates TGF-β1-dependent Smad3 phosphorylation and Dna binding. Has no effect on Smad2, p38 MAPK, ERK or PI 3-kinase signaling. Inhibits TGF-β1-induced myofibroblast differentiation of dermal fibroblasts. Also inhibits TGF-β2-induced endothelial cell differentiation in iPSCs.(In Vitro):(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.

(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.

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SIS3 HCl

TGF-beta/Smad

TGFBR

Smad3

Cancer

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521984-48-5

489.99

C28H27N3O3·HCl

>98% (HPLC)

DMSO: ≥ 30 mg/mL

O=C(N1CC2=C(C=C(OC)C(OC)=C2)CC1)/C=C/C3=C(C4=CC=CC=C4)N(C)C5=NC=CC=C53.[H]Cl

2-Propen-1-one, 1-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-, hydrochloride (1:1), (2E)-

(-20℃)

With Ice Pack

≥ 2 years