Smad3 Inhibitor, SIS3
- Product Name
- Smad3 Inhibitor, SIS3
- CAS No.
- 1009104-85-1
- Chemical Name
- Smad3 Inhibitor, SIS3
- Synonyms
- SIS3 ，S3552;SIS3 free base;Smad3 Inhibitor;(E/Z)-SIS3 free base;(Rac)-SIS3 free base;SMAD3 Inhibtor, SIS 3;Smad3 Inhibitor, SIS3;SIS-3 free base,SIS3 free base;(E)-1-(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-3-pyrrolo[2,3-b]pyridyl)-2-propen-1-one;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
- CBNumber
- CB22520818
- Molecular Formula
- C28H27N3O3
- Formula Weight
- 453.53
- MOL File
- 1009104-85-1.mol
Smad3 Inhibitor, SIS3 Property
- storage temp.
- Store at -20°C
- solubility
- DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS (pH 7.2) (1:3): 0.2 mg/ml
- form
- A crystalline solid
- color
- off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 15945
- Product name
- SMAD3 Inhibitor, SIS3
- Purity
- ≥98%
- Packaging
- 500μg
- Price
- $65
- Updated
- 2024/03/01
- Product number
- 15945
- Product name
- SMAD3 Inhibitor, SIS3
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $121
- Updated
- 2024/03/01
- Product number
- 15945
- Product name
- SMAD3 Inhibitor, SIS3
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $380
- Updated
- 2024/03/01
- Product number
- 466177
- Product name
- SMAD3 Inhibtor, SIS 3
- Packaging
- 2.5mg
- Price
- $425
- Updated
- 2021/12/16
- Product number
- S564500
- Product name
- SMAD3Inhibtor,SIS3
- Packaging
- 25mg
- Price
- $820
- Updated
- 2021/12/16
Smad3 Inhibitor, SIS3 Chemical Properties,Usage,Production
Uses
SMAD3 Inhibitor, SIS3 selectively inhibits TGF-β and activin. It has been shown to reduce TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.
Definition
ChEBI: An enamide resulting from the formal condensation of the amino group of 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline with the carboxy group of (2E)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)acrylic cid.
Biological Activity
Primary Target
TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling', 'The specific inhibitor of Smad3 (SIS3) is a pyrrolopyridine compound. 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. 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.
in vivo
E/Z-SIS3 free base (2 mg/kg, i.p.) inhibits smad3 phosphorylation and levels of TGF-β1, ameliorates bleomycin (BLM)-induced pulmonary fibrosis (PF) and inflammation in C57BL/6J mice[1].
| Animal Model: | BLM-induced PF in C57BL/6J mice[1] |
| Dosage: | 2 mg/kg |
| Administration: | i.p., every two days for 3 weeks |
| Result: | Inhibited the fibrosis and collagen deposition in lung. Reduced numbers of lymphocytes, macrophages, and neutrophils in bronchoalveolar Lavage (BAL). |