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566405

Sigma-Aldrich

SIS3

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

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

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About This Item

Empirical Formula (Hill Notation):
C28H27N3O3
CAS Number:
1009104-85-1
Molecular Weight:
453.53
MDL number:
MFCD24368989
UNSPSC Code:
12352200
NACRES:
NA.28
Pricing and availability is not currently available.

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.

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

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assay

≥90% (HPLC)

assay

≥95% (HPLC)

assay

≥95% (HPLC)

assay

≥97% (HPLC)

form

solid

form

solid

form

solid

form

lyophilized

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

solubility

DMSO: 15 mg/mL, ethanol: 5 mg/mL

solubility

water: 1 mg/mL

solubility

DMSO: 5 mg/mL (Use only fresh DMSO.), ethanol: 5 mg/mL

solubility

water: 1 mg/mL, DMSO: 5 mg/mL

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.[1] 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.[2]

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.[3] 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.[4][3] 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.[5]

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

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    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
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