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).
Synonyme(s) :
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
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About This Item
Formule empirique (notation de Hill):
C34H29N7O
Numéro CAS:
Poids moléculaire :
551.64
Code UNSPSC :
12352200
Niveau de qualité
Pureté
≥95% (HPLC)
Forme
solid
Fabricant/nom de marque
Calbiochem®
Conditions de stockage
OK to freeze
protect from light
Couleur
yellow
Solubilité
DMSO: 5 mg/mL
Conditions d'expédition
ambient
Température de stockage
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)
Clé InChI
BIWGYFZAEWGBAL-UHFFFAOYSA-N
Description générale
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.
Actions biochimiques/physiologiques
Cell permeable: yes
Primary Target
Akt1, Akt2, Akt3
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
Conditionnement
Packaged under inert gas
Avertissement
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
Autres remarques
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.
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.
Informations légales
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
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