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SIS3

Product Name
SIS3
CAS No.
521984-48-5
Chemical Name
SIS3
Synonyms
SIS3;CS-2236;SIS3 HCl;Caneritinib;SIS3 (SIS 3;SIS3 hydrochloride;SIS 3 HCL;SIS-3 HCL;Caneritinib(CI-1033);1,2,3,4-Tetrahydro-6,7-dimethoxy-2-[(2E)-3-(1-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-1-oxo-2-propenyl]-isoquinoline hydrochloride;(2E)-1-(6,7-Dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-propenone hydrochloride
CBNumber
CB5973013
Molecular Formula
C28H27N3O3HCl
Formula Weight
0
MOL File
521984-48-5.mol
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SIS3 Property

Melting point:
>161°C (dec.)
storage temp. 
2-8°C
solubility 
H2O: <2mg/mL
form 
powder
color 
yellow
InChIKey
CDKIEBFIMCSCBB-CALJPSDSSA-N
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
S0447
Product name
SIS3
Purity
≥98% (HPLC), powder
Packaging
5mg
Price
$411
Updated
2024/03/01
Tocris
Product number
5291
Product name
SIS3
Purity
≥98%(HPLC)
Packaging
50
Price
$1114
Updated
2021/12/16
Tocris
Product number
5291
Product name
SIS3
Purity
≥98%(HPLC)
Packaging
10
Price
$270
Updated
2021/12/16
TRC
Product number
T292310
Product name
1,2,3,4-Tetrahydro-6,7-dimethoxy-2-[(2E)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-1-oxo-2-propenyl]-isoquinolineMonohydrochloride
Packaging
1mg
Price
$95
Updated
2021/12/16
ApexBio Technology
Product number
B6096
Product name
SIS3
Packaging
5mg
Price
$103
Updated
2021/12/16
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SIS3 Chemical Properties,Usage,Production

Uses

Sugar insensitive 3 (SIS3) has been used as smad3?inhibitor in various cells.

Definition

ChEBI: SIS3 is a hydrochloride resulting from the reaction of SIS3 free base with 1 mol eq. of hydrogen chloride. It has a role as a Smad3 inhibitor. It contains a SIS3 free base(1+).

Biological Activity

sis3 is an inhibitor of smad3.the receptor-associated smads, such as smad2 and smad3, directly interact with activated tgf-receptor type i. smads form heteromeric complexes with smad4, which is a common mediator for all smad pathways.

Biochem/physiol Actions

Sugar insensitive 3 (SIS3) promotes drug-induced apoptosis and hinders the function of adenosine triphosphate (ATP)-binding cassette (ABC) transporter (ABCB1) and ABCG2. It resensitizes ABCB1 and ABCG2 overexpressed in cancerous cells, which contributes to chemotherapeutics.

in vitro

in the reporter assay, it was found that the increased luciferase activity of p3tp-lux could be abrogated by the sis3 treatment in a dosedependent manner. immunoprecipitation revealed sis3 attenuated the tgf-1-induced phosphorylation of smad3 and interaction of smad3 with smad4. whereas, sis3 did not affect the phosphorylation of smad2. in addition, it was found that sis3 attenuated the effects of tgf-1 by reducing the transcriptional activity. sis3 could also inhibit the myofibroblast differentiation of fibroblasts by tgf-1. moreover, sis3 diminished the constitutive phosphorylation of smad3 completely [1].

in vivo

animal study showed that, in tie2-cre;loxp-egfp mice, ages could induce endomt. immunoprecipitation and western blotting showed that smad3 could be activated by ages but was inhibited by sis3 in both mmecs and in stz-induced diabetic nephropathy. furthermore, confocal microscopy and real-time pcr showed that sis3 could abrogate endomt, reduce renal fibrosis, as well as retard nephropathy progression [2].

IC 50

3 μm

storage

Store at -20°C

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.
[2] li j et al. blockade of endothelial-mesenchymal transition by a smad3 inhibitor delays the early development of streptozotocin-induced diabetic nephropathy. diabetes.2010 oct;59(10):2612-24.

SIS3 Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from SIS3 manufacturers

Henan Aochuang Chemical Co.,Ltd.
Product
SIS3 521984-48-5
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
98%
Supply Ability
1Ton
Release date
2022-09-26
Career Henan Chemical Co
Product
SIS3 521984-48-5
Price
US $1.00/g
Min. Order
1g
Purity
99.99%
Supply Ability
200kg
Release date
2019-12-20

521984-48-5, SIS3Related Search:


  • SIS3
  • (2E)-1-(6,7-Dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-propenone hydrochloride
  • 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)-,hydrochloride (1:1), (2E)-
  • 1,2,3,4-Tetrahydro-6,7-dimethoxy-2-[(2E)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-1-oxo-2-propenyl]-isoquinoline Monohydrochloride
  • Caneritinib(CI-1033)
  • SIS3 hydrochloride
  • SIS3 HCl
  • SIS 3 HCL;SIS-3 HCL
  • 1,2,3,4-Tetrahydro-6,7-dimethoxy-2-[(2E)-3-(1-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-1-oxo-2-propenyl]-isoquinoline hydrochloride
  • Caneritinib
  • CS-2236
  • SIS3 (SIS 3
  • (E)-1-[6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl]-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one Hydrochloride
  • myofibroblast,inhibit,TGF-β1,TGF-beta/Smad,(E)SIS3,Smad3,(E)-SIS3,Transforming growth factor beta,fibroblasts,differentiation,(E) SIS3,phosphorylation,(E)-SIS-3,Inhibitor
  • 521984-48-5
  • C28H27N3O3HCl