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PF-4708671

ArtNr V0239-50mg
Hersteller InvivoChem LLC
CAS-Nr. 1255517-76-0
Menge 50 mg
Quantity options 100 mg 10 mg 250 mg 25 mg 500 mg
Kategorie
Typ Biochemicals
Specific against other
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Lieferbar
Description
InvivoChem Cat #:V0239CAS #:1255517-76-0Purity >=98%

Description: PF-4708671 is a novel, potent, highly specific and cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform)/RSK1 with potential antitumor activity. It inhibits RSK1 with a Ki/IC50 of 20 nM/160 nM in cell-free assays, exhibits 400-fold greater selectivity for S6K1 over S6K2, and displays 4- and > 20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. As the first S6K1-specific inhibitor reported, PF-4708671 showed potent antiproliferative activity in vitro and high antitumor efficacy in vivo by preventing the S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1), while having no effect upon the PMA-induced phosphorylation of substrates of the highly related RSK (p90 ribosomal S6 kinase) and MSK (mitogen- and stress-activated kinase) kinases.

Description: Description: PF-4708671 is a novel, potent, highly specific and cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform)/RSK1 with potential antitumor activity. It inhibits RSK1 with a Ki/IC50 of 20 nM/160 nM in cell-free assays, exhibits 400-fold greater selectivity for S6K1 over S6K2, and displays 4- and > 20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. As the first S6K1-specific inhibitor reported, PF-4708671 showed potent antiproliferative activity in vitro and high antitumor efficacy in vivo by preventing the S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1), while having no effect upon the PMA-induced phosphorylation of substrates of the highly related RSK (p90 ribosomal S6 kinase) and MSK (mitogen- and stress-activated kinase) kinases.

References:Biochem J. 2010 Oct 15; 431(2):245-55.

References:References:

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Alle Produkte sind nur für Forschungszwecke bestimmt. Nicht für den menschlichen, tierärztlichen oder therapeutischen Gebrauch.

Menge: 50 mg
Lieferbar: In stock
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