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About This Item
Empirical Formula (Hill Notation):
C20H21N3O2 · xHCl · yH2O
CAS Number:
Molecular Weight:
335.40 (anhydrous free base basis)
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Product Name
SB-505124 hydrochloride hydrate, ≥98% (HPLC)
Quality Level
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
yellow
solubility
DMSO: >10 mg/mL, H2O: insoluble
originator
GlaxoSmithKline
storage temp.
2-8°C
SMILES string
O.Cl.Cc1cccc(n1)-c2[nH]c(nc2-c3ccc4OCOc4c3)C(C)(C)C
InChI
1S/C20H21N3O2.ClH.H2O/c1-12-6-5-7-14(21-12)18-17(22-19(23-18)20(2,3)4)13-8-9-15-16(10-13)25-11-24-15;;/h5-10H,11H2,1-4H3,(H,22,23);1H;1H2
InChI key
DIDCCMVWCVRTNB-UHFFFAOYSA-N
Application
SB-505124 hydrochloride hydrate was used to study the role of TGF-β pathway in development and differentiation studies.3,4
Biochem/physiol Actions
SB-505124 is an inhibitor of activin receptor-like kinase (ALK) 5, also known as transforming growth factor-α type I receptor kinase, with an IC50 of 47 ± 5 nM.
SB-505124 selectively inhibits TGF-β type I receptors, activin receptor-like kinases (ALK) 4, 5 and 7. It inhibits ALK4-, 5- and 7-mediated activation of Smad2, Smad3 and MAPK pathway induced by TGF-β.1 SB-505124 inhibits the human fibroblast trans-differentiation induced by the co-culture with Esophageal squamous cell carcinoma.2
Features and Benefits
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
signalword
Warning
hcodes
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
target_organs
Respiratory system
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
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Related Content
Stacey DaCosta Byfield et al.
Molecular pharmacology, 65(3), 744-752 (2004-02-24)
Clinically, there is a great need for small molecule inhibitors that could control pathogenic effects of transforming growth factor (TGF-beta) and/or modulate effects of TGF-beta in normal responses. Inhibition of TGF-beta signaling would be predicted to enhance re-epithelialization of cutaneous
Kazuhiro Noma et al.
Gastroenterology, 134(7), 1981-1993 (2008-04-29)
Esophageal squamous cell carcinoma (ESCC) is known to be a highly angiogenic tumor. Here, we investigated the role of the stromal fibroblasts in the ESCC-induced angiogenic response using a novel 3-dimensional model. A novel assay was developed where cocultures of
Mary C Trask et al.
Developmental biology, 368(2), 273-282 (2012-06-07)
The ubiquitously expressed Polycomb Group protein Yin-Yang1 (YY1) is believed to regulate gene expression through direct binding to DNA elements found in promoters or enhancers of target loci. Additionally, YY1 contains diverse domains that enable a plethora of protein-protein interactions
Global Trade Item Number
| SKU | GTIN |
|---|---|
| S4696-25MG | 04061832434230 |
| S4696-5MG | 04061836928131 |
