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SMAD3

Names

[ CAS No. ]:
1009104-85-1

[ Name ]:
SMAD3

[Synonym ]:
IN1090
SMAD3 Inhibtor,SIS 3
(2E)-1-(6,7-Dimethoxy-3,4-dihydro-2(1H)-isoquinolinyl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-2-propen-1-one
2-Propen-1-one, 1-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-, (2E)-
1-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3-(1-methyl-2-phenylpyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one

Biological Activity

[Description]:

SIS3 free base is a potent and selective inhibitor of TGF- beta1-induced Smad3 phosphorylation with an IC50 of 3 μM. SIS3 free base increases luciferase activity of p3TP-lux by abrogating the overexpression of constitutively active form of ALK-5[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Stem Cell/Wnt >> TGF-beta/Smad
Signaling Pathways >> TGF-beta/Smad >> TGF-beta/Smad
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ALK

[Target]

Smad3, ALK-5[1]


[In Vitro]

SIS3 free base (0.3-10 μM; for 1 hour) attenuates the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4[1]. Western Blot Analysis[1] 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.

[References]

[1]. Jinnin M, et al. Characterization of SIS3, a novel specific inhibitor of Smad3, and its effect on transforming growth factor-beta1-induced extracellular matrix expression. Mol Pharmacol. 2006 Feb;69(2):597-607. Epub 2005 Nov 15.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
721.8±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C28H27N3O3

[ Molecular Weight ]:
453.532

[ Flash Point ]:
390.3±32.9 °C

[ Exact Mass ]:
453.205231

[ PSA ]:
56.59000

[ LogP ]:
5.28

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.628

Related Compounds