A pan Akt inhibitor (Ki = 160 pmol/L for all three isoforms) that interferes with mitotic progression and bipolar spindle formation; slows the progression of Akt-dependent tumors in vivo; concomitantly increases Akt Thr308 and Ser473 phosphorylation via a rapid feedback reaction

A-443654 – 5 mg

Brand:
Cayman
CAS:
552325-16-3
Storage:
-20
UN-No:
Non-Hazardous - /

Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival as well as angiogenesis. A-443654 is an inhibitor of Akt (Ki = 160 pmol/L for all three isoforms) that interferes with mitotic progression and bipolar spindle formation.{26942,26944} It induces G2/M accumulation, defects in centrosome separation, and formation of either monopolar arrays or disorganized spindles.{26944} A-443654 has been reported to slow the progression of Akt-dependent tumors in in vivo mouse models.{26942} In response to an A-443654-induced decrease in phosphorylation of Akt targets, a concomitant increase in Thr308 and Ser473 phosphorylation of Akt has been observed in human cancer cell lines.{26943} A-443654 has been used to examine the mechanism of this rapid feedback reaction.  

 

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Description

A pan Akt inhibitor (Ki = 160 pmol/L for all three isoforms) that interferes with mitotic progression and bipolar spindle formation; slows the progression of Akt-dependent tumors in vivo; concomitantly increases Akt Thr308 and Ser473 phosphorylation via a rapid feedback reaction

Formal name: αS-[[[5-(3-methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-1H-indole-3-ethanamine

Synonyms: 

Molecular weight: 397.5

CAS: 552325-16-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PKB/Akt||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

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