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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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SIS3 Suppliers

Tianjin Kailiqi Biotechnology Co., Ltd.
Tel
15076683720
Fax
022-23754520
Email
klq@cw-bio.com
Country
China
ProdList
4601
Advantage
55
Jiangsu Aikon Biopharmaceutical R&D co.,Ltd.
Tel
025-66099280 17798518460
Fax
(1)02557626880
Email
cfzhang@aikonchem.com
Country
China
ProdList
19915
Advantage
55
TOKYO CHEMICAL INDUSTRY CO., LTD.
Tel
03-36680489
Fax
03-3668-0520
Email
Sales-JP@TCIchemicals.com
Country
Japan
ProdList
28387
Advantage
80
TCI Europe
Tel
320-37350700
Fax
+32 (0)37350701
Email
sales@tcieurope.eu
Country
Europe
ProdList
23671
Advantage
75
Guangzhou Isun Pharmaceutical Co., Ltd
Tel
020-39119399 18927568969
Fax
020-39119999
Email
isunpharm@qq.com
Country
China
ProdList
4428
Advantage
55
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3466
Advantage
58
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
Shanghai JiYi Biotechnology Co. Ltd.
Tel
13621943973
Fax
-
Email
sales@shjiyipharmatech.com
Country
China
ProdList
1166
Advantage
55
Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Country
China
ProdList
51456
Advantage
80
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4512
Advantage
55
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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