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AKT inhibitor VIII Allosteric Akt kinase inhibitor

Catalog No.A3149
Size Price Stock Qty
10mM (in 1mL DMSO)
$130.00
In stock
10mg
$145.00
In stock
25mg
$350.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1.Eldad TZAHOR,Gabriele Matteo D'UVA,et al. "Methods, kits and devices for promoting cardiac regeneration." US Patent App. 15 ,2016.
2.D’Uva, Gabriele, et al. "ERBB2 triggers mammalian heart regeneration by promoting cardiomyocyte dedifferentiation and proliferation." Nature Cell Biology (2015). PMID:25848746

Quality Control

Chemical structure

AKT inhibitor VIII

Related Biological Data

AKT inhibitor VIII

Related Biological Data

AKT inhibitor VIII

Biological Activity

Description AKT inhibitor VIII is a potent and selective allosteric inhibitor of Akt kinase with IC50 values of 58 nM, 210 nM and 2119 nM, for Akt1, Akt2 and Akt3, respectively .
Targets Akt1 Akt2 Akt3      
IC50 58 nM 210 nM 2119 nM      

Protocol

Cell experiment [1]:

Cell lines

MCF-7 cell lines

Preparation method

The solubility of this compound in DMSO is >9.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10-100 μM for 24, 48, and 72 h

Applications

AKT inhibitor VIII significantly inhibited the proliferation and increased the LDH release in both cell lines in a dose-dependent manner. AKT inhibitor VIII dose-dependently induced cell cycle arrest at the G0/G1 phase. The protein expressions of p-cyclin D1, total cyclin D1, p-CDK2, total CDK2, pRb, total Rb, Bcl-xL, and Akt were significantly inhibited by AKT inhibitor VIII, whereas the protein expressions of Bad and Bax, and the proteolytic cleavage of caspase-9, caspase-7, and polyADP-ribose polymerase (PARP) were dramatically increased.

Animal experiment [1]:

Animal models

BALB/c nude mice

Dosage form

15 mg/kg and 30 mg/kg by intraperitoneal administration once daily for 8 days

Application

AKT inhibitor VIII dose-dependently suppressed the tumor growth in vivo, achieving 32% and 54% inhibition rates after intraperitoneal injection of 15 mg/kg and 30 mg/kg, respectively.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] [1] Zhong Z, 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.

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Chemical Properties

Cas No. 612847-09-3 SDF Download SDF
Synonyms N/A
Chemical Name 3-[1-[[4-(7-phenyl-3H-imidazo[4,5-g]quinoxalin-6-yl)phenyl]methyl]piperidin-4-yl]-1H-benzimidazol-2-one
Canonical SMILES C1CN(CCC1N2C3=CC=CC=C3NC2=O)CC4=CC=C(C=C4)C5=NC6=CC7=C(C=C6N=C5C8=CC=CC=C8)N=CN7
Formula C34H29N7O M.Wt 551.64
Solubility >9.2mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

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].

Reference:
[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.