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A6355

Sigma-Aldrich

3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione hydrochloride

powder, ≥98% (HPLC)

Synonyme(s) :

Erk Inhibitor

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About This Item

Formule empirique (notation de Hill):
C14H16N2O3S · HCl
Numéro CAS:
294675-79-9
Poids moléculaire :
328.81
Numéro MDL:
MFCD09038681
Code UNSPSC :
12352202
ID de substance PubChem :
24891079
Nomenclature NACRES :
NA.77
Le tarif et la disponibilité ne sont pas disponibles actuellement.

Niveau de qualité

100

Essai

≥98% (HPLC)

Forme

powder

Conditions de stockage

desiccated
under inert gas

Couleur

off-white

Solubilité

DMSO: ≥4 mg/mL

Température de stockage

2-8°C

Chaîne SMILES 

Cl[H].CCOc1ccc(cc1)C=C2SC(=O)N(CCN)C2=O

InChI

1S/C14H16N2O3S.ClH/c1-2-19-11-5-3-10(4-6-11)9-12-13(17)16(8-7-15)14(18)20-12;/h3-6,9H,2,7-8,15H2,1H3;1H/b12-9+;

Clé InChI

PQVLWVGMXJPJLG-NBYYMMLRSA-N

Application

3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione is an extracellular signal-regulated kinase (ERK) docking domain inhibitor. ERK inhibitors have been used to study traumatic brain injuries.

Actions biochimiques/physiologiques

3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione is extracellular signal-regulated kinase (ERK) docking domain inhibitor. Inhibits ERK binding rather then ERK activity at the ATP domain. IC50 = 25 μM in HeLa, A549, and SUM-159 tumor cells. Currently, no specific inhibitors of the ERK proteins exist. Preferentially binds to ERK2 with a Kd of ~5 μM and prevents its interaction with protein substrates. Shown to block ERK-mediated phosphorylation of ribosomal S6 kinase-1 (RSK-1) and ternary complex factor Elk-1, but exhibits little effect on ERK1/2 phosphorylation by MEK1/2.
Extracellular signal-regulated kinase (ERK) docking domain inhibitor. Inhibits ERK binding rather then ERK activity at the ATP domain. IC50 = 25 μM in HeLa, A549, and SUM-159 tumor cells.

Caractéristiques et avantages

This compound is featured on the MAPKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Certificats d'analyse (COA)

Lot/Batch Number
0000402773
0000402773
101M4628V
086K46075
086K46074

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Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

E Guerra et al.
Oncogene, 32(12), 1594-1600 (2012-05-09)
Our findings show that upregulation of a wild-type Trop-2 has a key controlling role in human cancer growth, and that tumour development is quantitatively driven by Trop-2 expression levels. However, little is known about the regulation of expression of the
Dexmedetomidine is neuroprotective in an in vitro model for traumatic brain injury
Schoeler, M., et al.
BMC Neurology, doi: 10-doi: 10 (2012)
Mikihito Kajiya et al.
Molecular pharmacology, 82(1), 115-124 (2012-04-19)
Muscarinic type 3 receptor (M3R) plays a pivotal role in the induction of glandular fluid secretions. Although M3R is often the target of autoantibodies in Sjögren's syndrome (SjS), chemical agonists for M3R are clinically used to stimulate saliva secretion in
Yiming Zhang et al.
The Journal of biological chemistry, 287(22), 18562-18572 (2012-04-12)
Although neuromedin U (NMU) has been implicated in analgesia, the detailed mechanisms still remain unclear. In this study, we identify a novel functional role of NMU type 1 receptor (NMUR1) in regulating the transient outward K(+) currents (I(A)) in small
Tony E Walshe et al.
Arteriosclerosis, thrombosis, and vascular biology, 29(8), 1185-1192 (2009-05-23)
Motivated by the central roles that vascular endothelial growth factor (VEGF) and transforming growth factor (TGF)-beta play in the assembly and maintenance of the vasculature, we examined the impact of systemic VEGF or TGF-beta signal inhibition on endothelial activation as
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