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Merck
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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.

别名:

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

经验公式(希尔记法):
C19H21F3N6
分子量:
390.41
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.28

品質等級

化驗

≥98% (HPLC)

形狀

solid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

off-white

溶解度

DMSO: 50 mg/mL, pale yellow

運輸包裝

ambient

儲存溫度

2-8°C

一般說明

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.

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C.) Stock solutions are stable for up to 6 months at -20°C.

其他說明

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

法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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