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559273 Sigma-AldrichS6K1 Inhibitor, PF-4708671 - Calbiochem

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

S6K1 Inhibitor, PF-4708671 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
分析证书
参考
Data Sheet

同义词: (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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概述

Replacement Information

重要规格表

Empirical Formula
C₁₉H₂₁F₃N₆

价格及供货情况

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Description
Overview	A cell-permeable piperazinyl-pyrimidine compound that acts as an inhibitor against S6K1 (K_i = 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.).
Catalogue Number	559273
Brand Family	Calbiochem®
Synonyms	(2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole, p70 Ribosomal S6 Kinase 1 Inhibitor

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

Product Information
Form	Off-white solid
Hill Formula	C₁₉H₂₁F₃N₆
Chemical formula	C₁₉H₂₁F₃N₆
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Purity	≥98% by HPLC

Physicochemical Information

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity	Standard Handling
Storage	+2°C to +8°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C.) Stock solutions are stable for up to 6 months at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
559273-10MGCN	04055977192339

Documentation

S6K1 Inhibitor, PF-4708671 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

S6K1 Inhibitor, PF-4708671 - Calbiochem 分析证书

标题	批号
559273	输入批号

参考

参考信息概述
Di, R., et al. 2012. Biochem. J. 441, 199. Pearce, L.R., et al. 2010. Biochem. J. 431, 245.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	17-July-2012 JSW
Synonyms	(2-((4-(5-Ethylpyrimidin-4-yl)piperazin-1-yl)methyl)-5-(trifluoromethyl)-1H-benzo[d]imidazole, p70 Ribosomal S6 Kinase 1 Inhibitor
Description	A cell-permeable piperazinyl-pyrimidine compound that acts as an inhibitor against S6K1 (K_i = 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 (Ser^235/236 and Ser^240/244), 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.
Form	Off-white solid
Intert gas (Yes/No)	Packaged under inert gas
Chemical formula	C₁₉H₂₁F₃N₆
Structure formula
Purity	≥98% by HPLC
Solubility	DMSO (50 mg/ml; pale yellow solution)
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C.) Stock solutions are stable for up to 6 months at -20°C.
Toxicity	Standard Handling
References	Di, R., et al. 2012. Biochem. J. 441, 199. Pearce, L.R., et al. 2010. Biochem. J. 431, 245.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > S6K Inhibitors

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