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324516

Sigma-Aldrich

A-484954

≥98% (HPLC), powder, eEF2K inhibitor, Calbiochem®

Synonyme(s) :

eEF2K Inhibitor, A-484954, 7-amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-6-carboxamide, Eukaryotic elongation factor-2 kinase inhibitor, A-484954

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About This Item

Formule empirique (notation de Hill):
C13H15N5O3
Numéro CAS:
142557-61-7
Poids moléculaire :
289.29
Numéro MDL:
MFCD22683836
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

product name

eEF2K Inhibitor, A-484954, The eEF2K Inhibitor, A-484954, also referenced under CAS 142557-61-7, controls the biological activity of eEF2K Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
protect from light

Couleur

off-white

Solubilité

DMSO: 2.5 mg/mL, clear, colorless

Conditions d'expédition

wet ice

Température de stockage

2-8°C

Chaîne SMILES 

O=C(C1=C(N2C3CC3)N=C(N)C(C(N)=O)=C1)N(CC)C2=O

InChI

1S/C13H15N5O3/c1-2-17-12(20)8-5-7(10(15)19)9(14)16-11(8)18(13(17)21)6-3-4-6/h5-6H,2-4H2,1H3,(H2,14,16)(H2,15,19)

Clé InChI

HWODCHXORCTEGU-UHFFFAOYSA-N

Description générale

A cell-permeable pyrido-pyrimidinedione derivative that acts as a highly potent and selective inhibitor of eukaryotic elongation factor-2 kinase (eEF2K) (IC50= 280 nM). Exhibits very little activity against a broad panel of serine/threonine and protein tyrosine kinases. Inhibits eEF2 phosphorylation in multiple cell lines tested without affecting the net eEF2 levels. At concentration where it inhibits eEF2K activity, it has no effect on the proliferation of cancer cell lines.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

Chen, Z., et al. 2011. J. Bio. Chem.286, 43951.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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

Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

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Consulter la Bibliothèque de documents

Megha Jhanji et al.
Nature communications, 13(1), 3244-3244 (2022-06-11)
Serum tyrosine levels increase during aging, neurocognitive, metabolic, and cardiovascular disorders. However, calorie restriction (CR) and sleep lower serum tyrosine levels. We previously showed that tyrosine inhibits tyrosyl-tRNA synthetase (TyrRS)-mediated activation of poly-ADP-ribose polymerase 1 (PARP1). Here, we show that
Sujata Jana et al.
Cancer cell, 41(5), 853-870 (2023-04-22)
We uncover a tumor-suppressive process in urothelium called transcriptional-translational conflict caused by deregulation of the central chromatin remodeling component ARID1A. Loss of Arid1a triggers an increase in a nexus of pro-proliferation transcripts, but a simultaneous inhibition of the eukaryotic elongation
Julie Pires Da Silva et al.
Cells, 9(2) (2020-02-16)
Many recent studies have demonstrated the involvement of endoplasmic reticulum (ER) stress in the development of cardiac diseases and have suggested that modulation of ER stress response could be cardioprotective. Previously, we demonstrated that the deacetylase Sirtuin 1 (SIRT1) attenuates

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