Molecular structure of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2, CAS Number: 612847-09-3
Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (CAS 612847-09-3)
See product citations (29)
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.
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SDS & Certificate of Analysis
Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 is a cell-permeable quinoxaline compound that may act 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 may act 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.
Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (CAS 612847-09-3) References
- Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors. | Barnett, SF., et al. 2005. Biochem J. 385: 399-408. PMID: 15456405
- Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. | Lindsley, CW., et al. 2005. Bioorg Med Chem Lett. 15: 761-4. PMID: 15664853
- Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors. | Zhao, Z., et al. 2005. Bioorg Med Chem Lett. 15: 905-9. PMID: 15686884
- Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members. | DeFeo-Jones, D., et al. 2005. Mol Cancer Ther. 4: 271-9. PMID: 15713898
- The neural progenitor-specifying activity of FoxG1 is antagonistically regulated by CKI and FGF. | Regad, T., et al. 2007. Nat Cell Biol. 9: 531-40. PMID: 17435750
- Characterization of a protein kinase B inhibitor in vitro and in insulin-treated liver cells. | Logie, L., et al. 2007. Diabetes. 56: 2218-27. PMID: 17563061
- Role of a novel PH-kinase domain interface in PKB/Akt regulation: structural mechanism for allosteric inhibition. | Calleja, V., et al. 2009. PLoS Biol. 7: e17. PMID: 19166270
- Oligomers of grape-seed procyanidin extract activate the insulin receptor and key targets of the insulin signaling pathway differently from insulin. | Montagut, G., et al. 2010. J Nutr Biochem. 21: 476-81. PMID: 19443198
- Akt phosphorylates Sec24: new clues into the regulation of ER-to-Golgi trafficking. | Sharpe, LJ., et al. 2011. Traffic. 12: 19-27. PMID: 20950345
- HER2 phosphorylation is maintained by a PKB negative feedback loop in response to anti-HER2 herceptin in breast cancer. | Gijsen, M., et al. 2010. PLoS Biol. 8: e1000563. PMID: 21203579
- Akt acutely activates the cholesterogenic transcription factor SREBP-2. | Luu, W., et al. 2012. Biochim Biophys Acta. 1823: 458-64. PMID: 22005015
- Resveratrol reduces steroidogenesis in rat ovarian theca-interstitial cells: the role of inhibition of Akt/PKB signaling pathway. | Ortega, I., et al. 2012. Endocrinology. 153: 4019-29. PMID: 22719052
- Counteracting autophagy overcomes resistance to everolimus in mantle cell lymphoma. | Rosich, L., et al. 2012. Clin Cancer Res. 18: 5278-89. PMID: 22879389
- Combining AKT inhibition with chloroquine and gefitinib prevents compensatory autophagy and induces cell death in EGFR mutated NSCLC cells. | Bokobza, SM., et al. 2014. Oncotarget. 5: 4765-78. PMID: 24946858
- The human parasite Leishmania amazonensis downregulates iNOS expression via NF-κB p50/p50 homodimer: role of the PI3K/Akt pathway. | Calegari-Silva, TC., et al. 2015. Open Biol. 5: 150118. PMID: 26400473
Inhibitor of:
AI314180, Akt1, Akt2, Akt3, ALG-4, ANGEL2, ANUBL1, ATF-7IP, BXDC2, C12orf39, C14orf162, C14orf39, C15orf39, C1orf86, C1QTNF (C1q and TNF related), C20orf151, C3orf54, CCDC9, CTRP2, D4Ertd22e, DENND1B, EVT-2, FAM170B, FLJ30851, GLT1D1, glycogen synthase 2, GnRHR2, IGSF3, KBTBD2, LOC728085, LRRC42, LTβR, MA3, MORG1, MTUS2, NAT-12, PFK-2 liv, PKNβ, PLEKHA6, PP2Cζ, PRR14, QIP1, QSER1, RBMY1E, RhebL1, Ser/Thr Protein Kinase, Ser/Thr protein phosphatase (PP2C), SerpinA3i, SGK2, STAC, Suppressin, Tap42, TAPT1, TBC1D1, TEF-4, THAP10, TRB-2, TRC8, WDR37, and YIPF6.Activator of:
14-3-3 σ, BC006779, BC1D14, Bcl-9L, Centaurin α2, Clm3, CTMP, eIF4E2, FKHRL1, GOLPH3, GTSF1, KIAA0240, KIAA0317, KLC1, LOC255809_AB124611, MARCKSL1, MNSF-β, MTSS1, PIK3IP1, Pleckstrin, PRL-1, RN-tre, SGK3, TELO2, TFG, TOB1, and TORC2.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2, 1 mg | sc-202048 | 1 mg | $204.00 | |||
Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2, 5 mg | sc-202048A | 5 mg | $265.00 |