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Key Documents

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S4696

Sigma-Aldrich

SB-505124 hydrochloride hydrate

≥98% (HPLC)

Sinónimos:

2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrochloride hydrate

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About This Item

Fórmula empírica (notación de Hill):
C20H21N3O2 · xHCl · yH2O
Número de CAS:
694433-59-5
Peso molecular:
335.40 (anhydrous free base basis)
MDL number:
MFCD11045901
UNSPSC Code:
12352200
PubChem Substance ID:
24724611
NACRES:
NA.77

Quality Level

100

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 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
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.

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.

pictograms

Exclamation mark
GHS07

signalword

Warning

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

target_organs

Respiratory system

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves

Certificados de análisis (COA)

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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
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
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
Liming Tan et al.
Neuron, 108(4), 735-747 (2020-10-23)
High acuity stereopsis emerges during an early postnatal critical period when binocular neurons in the primary visual cortex sharpen their receptive field tuning properties. We find that this sharpening is achieved by dismantling the binocular circuit present at critical period
Hongmin Yun et al.
Immunity, 53(5), 1050-1062 (2020-11-19)
Herpes simplex virus type 1 (HSV-1)-infected corneas can develop a blinding immunoinflammatory condition called herpes stromal keratitis (HSK), which involves the loss of corneal sensitivity due to retraction of sensory nerves and subsequent hyperinnervation with sympathetic nerves. Increased concentrations of
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