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Sigma-Aldrich

SIS3

≥90% (HPLC), solid, Smad3 inhibitor, Calbiochem®

Sinônimo(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

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About This Item

Fórmula empírica (Notação de Hill):
C28H27N3O3
Número CAS:
Peso molecular:
453.53
Código UNSPSC:
12352200
NACRES:
NA.28

product name

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.

Nível de qualidade

Ensaio

≥90% (HPLC)

forma

solid

fabricante/nome comercial

Calbiochem®

condição de armazenamento

OK to freeze
protect from light

cor

off-white

solubilidade

DMSO: 15 mg/mL
ethanol: 5 mg/mL

Condições de expedição

ambient

temperatura de armazenamento

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

chave InChI

IJYPHMXWKKKHGT-UHFFFAOYSA-N

Aplicação

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.

Ações bioquímicas/fisiológicas

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.

Embalagem

Packaged under inert gas

Advertência

Toxicity: Irritant (B)

Reconstituição

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

Outras notas

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

Informações legais

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

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 1

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


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Yi Luo et al.
Stem cell research & therapy, 15(1), 4-4 (2024-01-04)
TMC1 is one of the most common deafness genes causing DFNA36. Patient-derived human induced pluripotent stem cells (iPSCs) provide an opportunity to modelling diseases. TMC1 p.M418K mutation in human is orthologous to Beethoven mice. Here, we investigated the differentiation, morphology
Jeffery Grigsby et al.
Current eye research, 37(11), 1045-1053 (2012-08-22)
Acrolein has been implicated in retinal pigment epithelium (RPE) cell death, and has been associated with diabetic retinopathy. Our purpose was to investigate the potential effect of high glucose in influencing acrolein-mediated RPE cytokine production and cell death. We investigated
Xingli Ji et al.
Medical science monitor : international medical journal of experimental and clinical research, 24, 1633-1641 (2018-03-21)
BACKGROUND Fibrosis is the common pathological feature in most kinds of chronic kidney disease (CKD). TGF-β/Smads signaling is the master pathway regulating kidney fibrosis pathogenesis, in which Smad3 acts as the integrator of various pro-fibrosis signals. In this study, we
Chaitali Chakraborty et al.
Nature communications, 14(1), 6446-6446 (2023-10-14)
Chromatin organization controls transcription by modulating 3D-interactions between enhancers and promoters in the nucleus. Alterations in epigenetic states and 3D-chromatin organization result in gene expression changes contributing to cancer. Here, we map the promoter-enhancer interactome and regulatory landscape of glioblastoma
Masatoshi Jinnin et al.
Molecular pharmacology, 69(2), 597-607 (2005-11-17)
This is the first report that characterizes specific inhibitor of Smad3 (SIS3) as a potent and selective inhibitor of Smad3 function. In the reporter assay, the increased luciferase activity of p3TP-lux by the overexpression of constitutively active form of ALK-5

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