AKTI-1/2

Химические свойства

Pale Yellow Solid

Использование

AKTI-1/2 is a Allosteric Akt (PKB) inhibitors used in synergistic combination therapy for the treatment of cancer.

Ферментативный ингибитор

This dual Akt1/Akt2 inhibitor (FW = 551.64 g/mol; CAS 612847-09-3; Soluble to 20 mM in DMSO with gentle warming), also named 1,3- dihydro-1-[1-[[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]- methyl]-4-piperidinyl]-2H-benzimidazol-2-one, targets Protein kinase B (PKB) isoforms Akt1 (IC50 = 50 nM) and Akt2 (IC50 = 210 nM), serine/threonine-specific protein kinases that play a key role in multiple cellular processes such as glucose metabolism, apoptosis, cell proliferation, transcription and cell migration. Akti-1/2 is selective for Akt1 and 2 over a panel of other tyrosine and serine/threonine kinases. It also sensitizes LnCaP cells to TRAIL (TNF-related apoptosis-inducing ligand) induced apoptosis. Complete inhibition is achieved in liver cells treated with 1-10 μM. Akti-1/2 also blocks insulin regulation of PEP carboxykinase and glucose 6-phosphatase expression.