AKTI-1/2 Chemical Properties

Melting point:

242-245°C (dec.)

Density 

1.350±0.06 g/cm3(Predicted)

storage temp. 

Refrigerator

solubility 

insoluble in H2O; insoluble in EtOH; ≥9.2 mg/mL in DMSO

pka

7.49±0.50(Predicted)

form 

Yellow solid

color 

White to Yellow to Orange

CAS DataBase Reference

612847-09-3

AKTI-1/2 Usage And Synthesis

Chemical Properties

Pale Yellow Solid

Uses

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

Definition

ChEBI: 3-[1-[[4-(7-phenyl-3H-imidazo[4,5-g]quinoxalin-6-yl)phenyl]methyl]-4-piperidinyl]-1H-benzimidazol-2-one is a member of piperidines.

Biological Activity

akt inhibitor viii is a cell-permeable, reversible and potent, selective inhibitor of akt1, akt2 and akt3 with ic50 values of 58 nm, 210 nm and 2.12 μm, respectively.akt inhibitor viii has shown to remarkably increase anti-proliferation induced by furanodiene in human breast cancer cell mcf-7. akt inhibitor viii could enhance the furanodiene- stimulated akt and p-akt expression decreases as well as increase furanodiene-induced parp cleavage in mcf-7 cells [1].akt inhibitor viii has been revealed to inhibit igf-1-induced akt phosphorylation in a concentration-dependent manner. akt inhibitor viii has also been demonstrated to reduce pras40 phosphorylation in pc12 cells [2].

Enzyme inhibitor

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.

storage

Store at -20°C

References

[1] zhong z1, dang y, yuan x, guo w, li y, tan w, cui j, lu j, zhang q, chen x, wang y. furanodiene, a natural product, inhibits breast cancer growth both in vitro and in vivo. cell physiol biochem. 2012;30(3):778-90.
[2] wang h1, zhang q, zhang l, little pj, xie x, meng q, ren y, zhou l, gao g, quirion r, zheng w. insulin-like growth factor-1 induces the phosphorylation of pras40 via the pi3k/akt signaling pathway in pc12 cells. neurosci lett. 2012 may 10;516(1):105-9.

AKTI-1/2(612847-09-3)Related Product Information

• HYDROXY PENTOXIFYLLINE
• Cabozantinib
• Dacomitinib (PF299804)
• PLX4032
• Benzhydrylamine
• TPP
• N,N'-Diphenylurea
• Phenylphosphonic dichloride
• Dihydroxybenzoic acid
• 4'-Hydroxyacetophenone
• Xylene
• CC401 HCl
• Binimetinib
• BKM120 (NVP-BKM120, Buparlisib)
• Tivozanib
• (5-METHYL-1H-PYRAZOL-3-YL)-(2-PHENYLQUINAZOLIN-4-YL)AMINE
• 1,3-DIHYDRO-1-(1-((4-(6-PHENYL-1H-IMIDAZO[4,5-G]QUINOXALIN-7-YL)PHENYL)METHYL)-4-PIPERIDINYL)-2H-BENZIMIDAZOL-2-ONE TRIFLUOROACETATE SALT HYDRATE
• AKTI-1/2