SIS3

Names

[ CAS No. ]:
521984-48-5

[ Name ]:
SIS3

[Synonym ]:
(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 hydrochloride (1:1)
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)-, hydrochloride (1:1)

Biological Activity

[Description]:

SIS3 is a cell-permeable and selective inhibitor of Smad3. It inhibits Smad3 phosphorylation with an IC50 of 3 µM.

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> TGF-beta/Smad

Signaling Pathways >> TGF-beta/Smad >> TGF-beta/Smad

Research Areas >> Cancer

[References]

[1]. Boudreau HE et al. Wild-type and mutant p53 differentially regulate NADPH oxidase 4 in TGF-β-mediated migration of human lung and breast epithelial cells. Br J Cancer. 2014 May 13;110(10):2569-82.

[2]. 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.

[3]. Di Bernardini E et al. Endothelial lineage differentiation from induced pluripotent stem cells is regulated by microRNA-21 and transforming growth factor β2 (TGF-β2) pathways. J Biol Chem. 2014 Feb 7;289(6):3383-93.

[Related Small Molecules]

Chemical & Physical Properties

[ Boiling Point ]:
737.2ºC at 760 mmHg

[ Molecular Formula ]:
C₂₈H₂₈ClN₃O₃

[ Molecular Weight ]:
489.993

[ Flash Point ]:
399.7ºC

[ Exact Mass ]:
489.181915

[ PSA ]:
56.59000

[ LogP ]:
5.59550

[ Storage condition ]:
-20℃

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

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