124018

Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2

Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2, CAS 612847-09-3, is a cell-permeable, reversible inhibitor of Akt1/Akt2 (IC₅₀ = 58 nM, 210 nM, & 2.12 µM for Akt1, Akt2, and Akt3, respectively).

• Synonim(y): Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2, 1,3-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
• Wzór empiryczny (zapis Hilla): C₃₄H₂₉N₇O
• Numer CAS: 612847-09-3
• Masa cząsteczkowa: 551.64
• Kod UNSPSC: 12352200
• NACRES: NA.28

Właściwości

• Poziom jakości: 200
• Próba: ≥95% (HPLC)
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: yellow
• rozpuszczalność: DMSO: 5 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: 2-8°C
• InChI: 1S/C34H29N7O/c42-34-39-26-8-4-5-9-31(26)41(34)25-14-16-40(17-15-25)20-22-10-12-24(13-11-22)33-32(23-6-2-1-3-7-23)37-29-18-27-28(36-21-35-27)19-30(29)38-33/h1-13,18-19,21,25H,14-17,20H2,(H,35,36)(H,39,42)
• Klucz InChI: BIWGYFZAEWGBAL-UHFFFAOYSA-N

Opis

Opis ogólny

A 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.

A 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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
Akt1, Akt2, Akt3

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 58 nM, 210 nM, 2.12 µM against Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

Inne uwagi

Calleja, V., et al. 2009. PLoS Biol.7, e17.
Logie, L., et al. 2007. Diabetes56, 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.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable