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559273 S6K1 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.

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

559273
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₉H₂₁F₃N₆

Products

Catalogue NumberPackaging Qty/Pack
559273-10MG Glass bottle 10 mg
Description
OverviewA 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.).
Catalogue Number559273
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
ReferencesDi, R., et al. 2012. Biochem. J. 441, 199.
Pearce, L.R., et al. 2010. Biochem. J. 431, 245.
Product Information
FormOff-white solid
Hill FormulaC₁₉H₂₁F₃N₆
Chemical formulaC₁₉H₂₁F₃N₆
Structure formula ImageStructure formula Image
Quality LevelMQ100
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 InstructionsFollowing 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
Catalogue Number GTIN
559273-10MG 04055977192339

Documentation

S6K1 Inhibitor, PF-4708671 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

S6K1 Inhibitor, PF-4708671 - Calbiochem Certificates of Analysis

TitleLot Number
559273

References

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

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.

Revision17-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
DescriptionA 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.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₉H₂₁F₃N₆
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml; pale yellow solution)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C.) Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesDi, R., et al. 2012. Biochem. J. 441, 199.
Pearce, L.R., et al. 2010. Biochem. J. 431, 245.