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124018 Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 - CAS 612847-09-3 - Calbiochem

124018
Purchase on Sigma-Aldrich

Panoramica

Replacement Information

Tabella delle specifiche principali

Empirical FormulaCAS #
C₃₄H₂₉N₇O 612847-09-3

Products

Numero di catalogoConfezionamento Qtà/conf
124018-1MG Fiala di plastica 1 mg
124018-5MG Bottiglia di vetro 5 mg
Description
OverviewA cell-permeable and reversible quinoxaline compound that potently and selectively inhibits Akt1/Akt2 activity (IC50 = 58 nM, 210 nM, and 2.12 µM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition appears to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 µM. Overcomes Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and is shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 both in cultured cells in vitro and in mice in vivo. A 10 mM (1 mg/181 µl) solution of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (Cat. No. 124017) in DMSO is also available.
Catalogue Number124018
Brand Family Calbiochem®
Synonyms1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one, Akti-1/2
References
ReferencesCalleja, V., et al. 2009. PLoS Biol. 7, e17.
Logie, L., et al. 2007. Diabetes 56, 228.
Barnett, S.F., et al. 2005. Biochem. J. 385, 399.
DeFeo-Jones, D., et al. 2005. Mol. Cancer Ther. 4, 271.
Zhao, Z., et al. 2005. Bioorg. Med. Chem. Lett. 15, 905.
Lindsley, C.W., et al. 2005. Bioorg. Med. Chem. Lett. 15, 761.
Product Information
CAS number612847-09-3
ATP CompetitiveN
FormYellow solid
Hill FormulaC₃₄H₂₉N₇O
Chemical formulaC₃₄H₂₉N₇O
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ200
Applications
ApplicationAkt Inhibitor VIII, Isozyme-Selective, Akti-1/2, CAS 612847-09-3, is a cell-permeable, reversible & selective inhibitor of Akt1/Akt2 (IC50 = 58 nM and 210 nM for Akt1 & Akt2, respectively),
Biological Information
Primary TargetAkt1, Akt2, Akt3
Primary Target IC<sub>50</sub>58 nM, 210 nM, 2.12 µM against Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
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 (-70°C). Stock solutions are stable for up to 6 months at -70°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 - CAS 612847-09-3 - Calbiochem MSDS

Titolo

Scheda di sicurezza (MSDS) 

Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 - CAS 612847-09-3 - Calbiochem Certificati d'Analisi

TitoloNumero di lotto
124018

Riferimenti bibliografici

Panoramica delle referenze
Calleja, V., et al. 2009. PLoS Biol. 7, e17.
Logie, L., et al. 2007. Diabetes 56, 228.
Barnett, S.F., et al. 2005. Biochem. J. 385, 399.
DeFeo-Jones, D., et al. 2005. Mol. Cancer Ther. 4, 271.
Zhao, Z., et al. 2005. Bioorg. Med. Chem. Lett. 15, 905.
Lindsley, C.W., et al. 2005. Bioorg. Med. Chem. Lett. 15, 761.

Brochure

Titolo
Akt
Scheda tecnica

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.

Revision22-September-2012 JSW
Synonyms1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one, Akti-1/2
DescriptionA cell-permeable, reversible, potent, and selective inhibitor of Akt1/Akt2 activity (IC50 = 58 nM, 210 nM, and 2.12 µM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition is reported to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 µM. Overcomes Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and is shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 both in cultured cells in vitro and in mice in vivo.
FormYellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number612847-09-3
Chemical formulaC₃₄H₂₉N₇O
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (5 mg/ml)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
Toxicity Standard Handling
ReferencesCalleja, V., et al. 2009. PLoS Biol. 7, e17.
Logie, L., et al. 2007. Diabetes 56, 228.
Barnett, S.F., et al. 2005. Biochem. J. 385, 399.
DeFeo-Jones, D., et al. 2005. Mol. Cancer Ther. 4, 271.
Zhao, Z., et al. 2005. Bioorg. Med. Chem. Lett. 15, 905.
Lindsley, C.W., et al. 2005. Bioorg. Med. Chem. Lett. 15, 761.