475988 Sigma-AldrichmTOR Inhibitor III, PP242 - Calbiochem
The mTOR Inhibitor III, PP242 controls the biological activity of mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
More>> The mTOR Inhibitor III, PP242 controls the biological activity of mTOR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Less<<mTOR Inhibitor III, PP242 - Calbiochem: SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.
Synonyme: 2-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol, Dihydrate, TORKinib, mTOR Inhibitor III, PP242
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Übersicht
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Key Spec Table
| Empirical Formula |
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| C₁₆H₁₆N₆O • 2H₂O |
Preis & Verfügbarkeit
| Bestellnummer | Verfügbarkeit | Verpackung | St./Pkg. | Preis | Menge | |
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| 475988-5MG |
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5 mg |
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| Description | |
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| Overview | A cell-permeable pyrazolopyrimidine compound that acts as a potent, reversible, and ATP-competitive inhibitor against both mTORC1 & mTORC2 (IC50 = 30 & 58 nM, respectively, with 100 µM ATP). PP242 inhibits PKCα, p110γ, and JAK2 with 6-, 13-, and 14-fold less potency and exhibits much reduced or no activity against a panel of 216 other kinases at a concentration of 1 µM (maximum of 68% or 77% inhibition observed with 10 or 100 µM ATP, respectively). PP242 differentially inhibits insulin-stimulated phosphorylations of cellular proteins both in cultures (2.5 µM) in vitro and in mice (20 mg/kg i.p.) in vivo in a manner distinctly different from that seen in mTORC2-functional knockout SIN1-/- cells or in cultures treated with Rapamycin (Cat. Nos. 553210, 553211, 553212), which targets only mTORC1, but not mTORC2. Blockage of 4EBP1 T36/T45/S65 phosphorylation by PP242 upon insulin stimulation in primary MEFs correlates well with an enhanced 4EBP1 association with the cap-binding protein eIF4E, resulting in a selective inhibition of cap-dependent, but not cap-independent, protein translation. |
| Catalogue Number | 475988 |
| Brand Family | Calbiochem® |
| Synonyms | 2-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol, Dihydrate, TORKinib, mTOR Inhibitor III, PP242 |
| References | |
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| References | Feldman, M.E., et al. 2009. PLoS Biology 7, 391. Apsel, B., et al. 2008. Nat. Chem. Biol. 4, 691. |
| Product Information | |
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| Form | Off-white solid |
| Hill Formula | C₁₆H₁₆N₆O • 2H₂O |
| Chemical formula | C₁₆H₁₆N₆O • 2H₂O |
| Structure formula Image | |
| Quality Level | MQ100 |
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| Biological Information | |
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| Purity | ≥97% by HPLC |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
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| Specifications |
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| Global Trade Item Number | |
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| Bestellnummer | GTIN |
| 475988-5MG | 04055977184396 |
Documentation
mTOR Inhibitor III, PP242 - Calbiochem SDB
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mTOR Inhibitor III, PP242 - Calbiochem Analysenzertifikate
| Titel | Chargennummer |
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| 475988 |
Literatur
| Übersicht |
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| Feldman, M.E., et al. 2009. PLoS Biology 7, 391. Apsel, B., et al. 2008. Nat. Chem. Biol. 4, 691. |
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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.
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