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559273

Sigma-Aldrich

S6K1 Inhibitor, PF-4708671

The S6K1 Inhibitor, PF-4708671 controls the biological activity of S6K1. This small molecule/inhibitor is primarily used for Cancer applications.

Synonyme(s) :

S6K1 Inhibitor, PF-4708671, (2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole, p70 Ribosomal S6 Kinase 1 Inhibitor

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About This Item

Formule empirique (notation de Hill):
C19H21F3N6
Poids moléculaire :
390.41
Numéro MDL:
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.28

Niveau de qualité

Pureté

≥98% (HPLC)

Forme

solid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
protect from light

Couleur

off-white

Solubilité

DMSO: 50 mg/mL, pale yellow

Conditions d'expédition

ambient

Température de stockage

2-8°C

Description générale

A cell-permeable piperazinyl-pyrimidine compound that acts as an inhibitor against S6K1 (Ki = 20 nM; IC50 = 160 nM) and MSK1 (IC50 = 950 nM) kinase activity, exhibiting little or much reduced potency against 85 other protein and lipid kinases (IC50 = 4.7, 9.2, 65 µM, respectively, against RSK1, RSK2, and S6K2; ≤27% inhibition of the rest at 1 µM). Shown to selectively inhibit IGF1- and PMA-stimulated S6K1 substrates phosphorylation in HEK-293 cells in a dose-dependent manner (up to 10 µM) in vitro and alleviate heart remodeling and functional damage in a MI (myocardial infarction) model in mice in vivo (75/mg/kg/daily i.p.).
A cell-permeable piperazinyl-pyrimidine compound that acts as an inhibitor against S6K1 (Ki = 20 nM; IC50 = 160 nM) and MSK1 (IC50 = 950 nM) kinase activity, exhibiting little or much reduced potency against a panel of 75 other protein kinases (IC50 = 4.7, 9.2, 65 µM, respectively, against RSK1, RSK2, and S6K2; ≤27% inhibition of the rest at 1 µM) and 10 lipid kinases (≤6% inhibition at 10 µM). Inhibits IGF1-induced phosphorylation of cellular S6K1 substrates S6 (Ser235/236 and Ser240/244), mTOR (Ser2448), and Rictor (Thr1135) in serum-starved HEK-293 cultures, but not the phoshorylation of MSK or RSK cellular substrates (CREB Ser133 and GSK3α/β Ser21/ Ser9, respectively) upon PMA stimulation even at concentrations as high as 10 µM. Inhibition of S6K1 activation by rapamycin (Cat. Nos. 553210, 553211, & 553212) or S6K1 activity by PF-4708671 (75/mg/kg/daily i.p.) are both shown to alleviate heart remodeling and functional damage following left coronary artery ligation-induced MI (myocardial infarction) in mice in vivo. Cellular PF-4708671 treatment is also reported to result in increased S6K1 phosphorylation, likely due to a blockage of down-stream negative feedback mechanism.

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 6 months at -20°C.

Autres remarques

Di, R., et al. 2012. Biochem. J.441, 199.
Pearce, L.R., et al. 2010. Biochem. J.431, 245.

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


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