Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 CAS: 612847-09-3
MF: C34H29N7O
MW: 551.64

Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (CAS 612847-09-3)

Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 | CAS 612847-09-3 is rated 5.0 out of 5 by 1.
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Alternate Names: Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 is also known as Akt Inhibitor VIII trifluoroacetate salt hydrate.
Application: Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 is a potent and selective inhibitor of Akt1/2, and mild inhibitor of Akt3.
CAS Number: 612847-09-3
Purity: ≥95%
Molecular Weight: 551.64
Molecular Formula: C34H29N7O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity (IC50 = 58 nM, 210 nM, and 2.12 μM; respectively). Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 does not exhibit any inhibitory effect against pleckstrin homology (PH) domain-lacking Akts, AGC family kinases, PKA, PKC or SGK. Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 prevails over Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and has been shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 in cultured cells and in mice. Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 is cell permeable, blocking insulin regulation of forkhead box 01 activity at 1 µM in rat hepatoma cells. Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 is also known as 1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one.


References

1. Barnett, S.F., et al. 2005. Biochem. J. 385: 399-408. PMID: 15456405

2. Lindsley, C.W., et al. 2005. Bioorg. Med. Chem. Lett. 15: 761-764. PMID: 15664853

3. Zhao, Z., et al. 2005. Bioorg. Med. Chem. Lett. 15: 905-909. PMID: 15686884

4. DeFeo-Jones, D., et al. 2005. Mol. Cancer Ther. 4: 271-279. PMID: 15713898

5. Logie, L., et al. 2007. Diabetes. 56: 2218-2227. PMID: 17563061

6. Calleja, V., et al. 2009. PLoS Biol. 7: e17. PMID: 19166270

Physical State :
Solid
Solubility :
Soluble in DMSO (5 mg/ml), and methanol.
Storage :
Store at room temperature
Melting Point :
>255° C (dec.)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.73 (Predicted)
IC50 :
Akt1: IC50 = 58 nM; Akt2: IC50 = 210 nM; Akt3: IC50 = 2.12 µM; PKA: IC50 = 50 µM; PKC: IC50 = 50 µM; SGK: IC50 = 50 µM
pK Values :
pKa: 7.49 (Predicted), pKb: 7.97 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
SMILES :
C1CN(CCC1N2C3=CC=CC=C3NC2=O)CC4=CC=C(C=C4)C5=NC6=CC7=C(C=C6N=C5C8=CC=CC=C8)N=CN7

Download SDS (MSDS)

Certificate of Analysis

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Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (CAS 612847-09-3)  Product Citations

See how others have used Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (CAS 612847-09-3). Click on the entry to view the PubMed entry .

Citations 1 to 10 of 25 total

PMID: # 34321276  Lu, YC.|Zheng, Z.|Lowery, FJ.|Gartner, JJ.|Prickett, TD.|Robbins, PF.|Rosenberg, SA.| et al. 2021. J Immunother Cancer. 9:

PMID: # 30065026  Stallaert, W. et al. 2018. Sci Signal. 11:

PMID: # 29652795  Pasquereau, S. et al. 2018. Viruses. 10:

PMID: # 27412556  Jang, H. et al. 2016. Nat Commun. 7: 12180.

PMID: # 27150024  Tsuji, S. et al. 2016. J. Vet. Med. Sci.

PMID: # 27076174  Kumar, A. et al. 2016. Sci Rep. 6: 24090.

PMID: # 27620179  Zhao, D.|Yang, LY.|Wang, XH.|Yuan, SS.|Yu, CG.|Wang, ZW.|Lang, JN.|Feng, YM.| et al. 2016. Cardiovasc Diabetol. 15: 132.

PMID: # 25885538  Selvaraj, N. et al. 2015. Cell Commun. Signal. 13: 12.

PMID: # 26400473  Calegari-Silva, TC. et al. 2015. Open Biol. 5: 150118.

PMID: # 26151859  Retamales, A. et al. 2015. Biochem. Biophys. Res. Commun. 464: 596-602.

Citations 1 to 10 of 25 total
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Rated 5 out of 5 by from Wang Wang, D. et al. (PubMed 26159568) found that Akti-1/2 (Akt Inhibitor VIII, Isozyme-Selective) and Dorsomorphon (sc-361173) reduced the influence of naringin on -catenin phosphorylation, suggesting naringin activates -catenin via regulating Akt and AMPK. -SCBT Publication Review
Date published: 2015-02-12
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