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Key Documents

S4696

Sigma-Aldrich

SB-505124 hydrochloride hydrate

≥98% (HPLC)

Synonym(s):

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

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20 MG
CN¥1,370.70

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20 MG
CN¥1,370.70

About This Item

Empirical Formula (Hill Notation):
C20H21N3O2 · xHCl · yH2O
CAS Number:
Molecular Weight:
335.40 (anhydrous free base basis)
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77

CN¥1,370.70


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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

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This Item
T2011T2327650357
biological source

chicken egg white

biological source

chicken egg white

biological source

Glycine max (soybean)

biological source

-

Quality Level

200

Quality Level

300

Quality Level

200

Quality Level

300

form

powder

form

powder

form

lyophilized powder

form

lyophilized solid

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

solubility

water: soluble 10 g/L

solubility

water: soluble 10 g/L

solubility

-

solubility

67 mM potassium phosphate buffer, pH 7.6: 5 mg/mL

mol wt

14 kDa

mol wt

14 kDa

mol wt

-

mol wt

-

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.

Pictograms

Exclamation mark

Signal Word

Warning

Hazard Statements

Hazard Classifications

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

Target Organs

Respiratory system

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

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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
    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
    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
    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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