Merck
  • 566405
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566405

Sigma-Aldrich

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:
Molecular Weight:
453.53

品質水準

アッセイ

≥90% (HPLC)

形状

solid

manufacturer/tradename

Calbiochem®

保管条件

OK to freeze
protect from light

off-white

溶解性

DMSO: 15 mg/mL
ethanol: 5 mg/mL

輸送温度

ambient

保管温度

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

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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.

Sigma-Aldrich

566405

Smad3 Inhibitor, SIS3

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Sigma-Aldrich

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SOD1 Inhibitor, LCS-1

Src Inhibitor, PP1 The Src Inhibitor PP1, also referenced under CAS 172889-26-8, controls the biological activity of Src. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Millipore

567809-M

Src Inhibitor, PP1

MK2a Inhibitor The MK2a Inhibitor, also referenced under CAS 41179-33-3, controls the biological activity of MK2a. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Sigma-Aldrich

475863

MK2a Inhibitor

assay

≥90% (HPLC)

assay

≥99% (HPLC)

assay

≥98% (HPLC)

assay

≥95% (HPLC)

form

solid

form

solid

form

solid

form

solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze

storage condition

OK to freeze, protect from light

color

off-white

color

white

color

off-white

color

pale yellow

solubility

DMSO: 15 mg/mL, ethanol: 5 mg/mL

solubility

DMSO: 50 mg/mL, clear, colorless

solubility

DMSO: 25 mg/mL

solubility

DMSO: 5 mg/mL, ethanol: 5 mg/mL

アプリケーション

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.

生物化学的/生理学的作用

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.

包装

Packaged under inert gas

警告

Toxicity: Irritant (B)

再構成

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

その他情報

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

法的情報

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

保管分類コード

11 - Combustible Solids

WGK

WGK 1

引火点(°F)

Not applicable

引火点(℃)

Not applicable

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