SIS3

SKU: orb1224814

Description

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.

Key Properties

• CAS Number: 521984-48-5
• MW: 489.99
• Purity: >98% (HPLC)
• Formula: C₂₈H₂₇N₃O₃·HCl
• SMILES: 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
• Target: TGFBR
• Solubility: DMSO: ≥ 30 mg/mL

Bioactivity

• 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SIS3 HCl

Quick Database Links

Gene Symbol

TGFBR