566405

Smad3 Inhibitor, SIS3

Smad3 Inhibitor, SIS3, CAS 1009104-85-1, is a cell-permeable, selective inhibitor of TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated signaling. Does not affect Smad2, MAPK, ERK, or PI3-K.

• Synonym(s): Smad3 Inhibitor, SIS3, SIS3, 6,7-Dimethoxy-2-((2E)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl-prop-2-enoyl))-1,2,3,4-tetrahydroisoquinoline, Specific Inhibitor of Smad 3
• Empirical Formula (Hill Notation): C₂₈H₂₇N₃O₃
• CAS Number: 1009104-85-1
• Molecular Weight: 453.53
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥90% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 15 mg/mL; ethanol: 5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C28H27N3O3/c1-30-27(19-8-5-4-6-9-19)22(23-10-7-14-29-28(23)30)11-12-26(32)31-15-13-20-16-24(33-2)25(34-3)17-21(20)18-31/h4-12,14,16-17H,13,15,18H2,1-3H3
• InChI key: IJYPHMXWKKKHGT-UHFFFAOYSA-N

Description

Application

The specific inhibitor of Smad3 (SIS3) has been used to block transforming growth factor (TGF)-β/ mothers against decapentaplegic homolog 3 (SMAD3) signaling to characterize the signaling pathways that contribute to the activation of signal transducer and activator of transcription 3 (STAT3) in lung fibroblasts. It has also been used as a SMAD3 inhibitor in serum-free media to assess its ability to prevent the acrolein effect in ARPE-19 cells.

Biochem/physiol Actions

Primary Target
TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling

The specific inhibitor of Smad3 (SIS3) is a pyrrolopyridine compound. It selectively blocks transforming growth factor (TGF)-β1-dependent mothers against decapentaplegic homolog 3 (Smad3) phosphorylation and Smad3-mediated cellular pathway without affecting Smad2, p38 mitogen-activated protein kinase (MAPK), extracellular-signal-regulated kinase (ERK), or phosphoinositide 3-kinase (PI3K) signaling. Through its inhibitory function, SIS3 regulates fibrosis, apoptosis, and inflammation in mouse unilateral ureteral obstruction (UUO) kidneys. Therefore, SIS3 can be an effective drug in further anti-fibrosis treatment of kidney disease.

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Reversible: no
Product does not compete with ATP.
Cell permeable: yes
Jinnin, M., et al. 2006. Mol. Pharmacol.69, 597.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable