CAS 694433-59-5|SB505124

Introduction：Basic information about CAS 694433-59-5|SB505124, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. SB505124 BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

Common Name	SB505124
CAS Number	694433-59-5	Molecular Weight	335.400
Density	1.2±0.1 g/cm3	Boiling Point	509.7±50.0 °C at 760 mmHg
Molecular Formula	C₂₀H₂₁N₃O₂	Melting Point	/
MSDS	/	Flash Point	180.5±20.4 °C

Names

Name	2-[4-(1,3-benzodioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl]-6-methylpyridine
Synonym	More Synonyms

SB505124 BiologicalActivity

Description	SB-505124 is a selective inhibitor of TGFβR with IC50 of 129 nM and 47 nM for ALK4, ALK5, respectively, and it does not inhibits ALK1, 2, 3, or 6 but ALK7.
Related Catalog	Signaling Pathways >>TGF-beta/Smad >>TGF-β ReceptorResearch Areas >>Cancer
Target	IC50: 129 nM (ALK4), 47 nM (ALK5)
In Vitro	SB-505124 demonstrates no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC50 value of 129±11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 μM. SB-505124 (1 μM) inhibits the TGF-β-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB-505124 (1 or 5 μM) potently inhibits TGF-β-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells[1]. SB-505124 (10 µM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro[2]. SB-505124 susspresses CTGF and α-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB-505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC[3].
Kinase Assay	Briefly, phospho-p38 is immunoprecipitated from 200 μg of cell lysates with an immobilized phosphor-p38 antibody overnight at 4°C. p38 kinase activity is measured using 2 μg of ATF-2 fusion protein as the substrate with addition of 200 μM ATP. After a 30-min incubation at 30°C, the reaction is terminated with LaemmLi sample buffer, and the proteins are boiled and resolved by 10% SDS-polyacrylamide gel electrophoresis, transferred to nitrocellulose membrane, and immunoblotted with phospho-ATF-2 antibody.
Cell Assay	Cell viability is measured as described previously or by using the modified tetrazolium salt WST-1. Approximately 2000 cells are seeded in 96-well dishes in 100 μL of 0.2% FBS phenol red-free media overnight. The cells are treated with 50 μL of SB-505124 (to achieve the final concentrations indicated) for 30 min before being treated with or without TGF-β1 and TNF-α to a final volume of 200 μL. Cell growth is measured at the indicated time points by incubating each well with 10 μL of WST-1 for 3 h at 37°C. Metabolically active cells cleave WST-1 to water-soluble formazan, which is directly quantitated with an enzyme-linked immunosorbent assay plate reader. Each experiment is done at least twice, and treatment for each cell line is done in triplicate.
References	[1]. DaCosta Byfield S, et al. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2004 Mar;65(3):744-52. [2]. Sutariya V, et al. Thermoreversible gel for delivery of activin receptor-like kinase 5 inhibitor SB-505124 for glaucoma filtration surgery. Pharm Dev Technol. 2013 Jul-Aug;18(4):957-62. [3]. Sapitro J, et al. Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by activin receptor-like kinase 5 inhibitor. Mol Vis. 2010 Sep 16;16:1880-92.

Chemical & Physical Properties

Density	1.2±0.1 g/cm3
Boiling Point	509.7±50.0 °C at 760 mmHg
Molecular Formula	C₂₀H₂₁N₃O₂
Molecular Weight	335.400
Flash Point	180.5±20.4 °C
Exact Mass	335.163391
PSA	60.03000
LogP	4.77
Appearance of Characters	yellow
Vapour Pressure	0.0±1.3 mmHg at 25°C
Index of Refraction	1.600
InChIKey	WGZOTBUYUFBEPZ-UHFFFAOYSA-N
SMILES	Cc1cccc(-c2[nH]c(C(C)(C)C)nc2-c2ccc3c(c2)OCO3)n1
Storage condition	2-8°C
Water Solubility	DMSO: >10mg/mL

Safety Information

Hazard Codes	Xi
Risk Phrases	36/37/38
Safety Phrases	26-36
HS Code	29349990

Synonyms

Pyridine, 2-[4-(1,3-benzodioxol-5-yl)-2-(1,1-dimethylethyl)-1H-imidazol-5-yl]-6-methyl-

2-[4-(1,3-benzodioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl]-6-methylpyridine

SB 505124

2-[4-(1,3-Benzodioxol-5-yl)-2-(2-methyl-2-propanyl)-1H-imidazol-5-yl]-6-methylpyridine

SB-505124

SB505124

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