A-443654 - CAS 552325-16-3
Catalog number: 552325-16-3
Category: Inhibitor
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A-443654 is a potent small-molecule inhibitor of all three Akt serine/threonine kinases, induces Akt Ser-473 phosphorylation in all human cancer cell lines tested, including PTEN- and TSC2-deficient lines. It inhibits Akt-dependent signal transduction in cells and in vivo in a dose-responsive manner.
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1.Akt inhibitors induce apoptosis in chronic lymphocytic leukemia cells.
de Frias M;Iglesias-Serret D;Cosialls AM;Coll-Mulet L;Santidrián AF;González-Gironès DM;de la Banda E;Pons G;Gil J Haematologica. 2009 Dec;94(12):1698-707. doi: 10.3324/haematol.2008.004028. Epub 2009 Oct 8.
BACKGROUND: ;The phosphatidylinositol-3-kinase/Akt pathway has been described to be critical in the survival of chronic lymphocytic leukemia cells. In this study we analyzed the effect of two selective chemical inhibitors of Akt (Akti-1/2 and A-443654) on the survival of chronic lymphocytic leukemia cells.;DESIGN AND METHODS: ;Using cytometry we studied the cytotoxic effects of Akt inhibitors on peripheral B and T lymphocytes from patients with chronic lymphocytic leukemia and from healthy donors. We studied the changes induced by Akti-1/2 and A-443654 at the mRNA level by performing reverse transcriptase multiplex ligation-dependent probe amplification. We also studied the changes induced by both Akt inhibitors in some BCL-2 protein family members on chronic lymphocytic leukemia cells by western blotting. Moreover, we analyzed the cytotoxic effect of Akt inhibitors in patients' cells with deleted/mutated TP53.;RESULTS: ;Both inhibitors induced apoptosis in chronic lymphocytic leukemia cells in a dose-dependent manner. Moreover, B cells from patients with chronic lymphocytic leukemia were more sensitive to Akt inhibitors than T cells from leukemic patients, and B or T cells from healthy donors.
2.[Effects of insulin and LY294002 inhibitors of PI3K on the regulations and expression of aquaporin 9 in normal liver cells].
Liu H;Mei ZC;Xiao X Zhonghua Gan Zang Bing Za Zhi. 2010 Jun;18(6):455-8. doi: 10.3760/cma.j.issn.1007-3418.2010.06.014.
OBJECTIVES: ;To explore the effects of insulin on the expression and the regulatory pathway of AQP9 in normal human liver cells.;METHODS: ;Normal human liver cells L02 were cultured and treated with PI3K inhibitor LY294002, AKT inhibitor A-443654, MAPK inhibitors SB2030580 and insulin at different concentrations respectively. The AQP9 mRNA and protein expressions were detected with semi-quantitative RT-PCR and Western blot respectively.;RESULTS: ;The insulin (100 nmol/L approximately 500 nmol/L) treatment decreased the expression of AQP9 in normal human liver cells (P less than 0.05) concentration dependently, and the expression of AQP9 began to reduce from 3 hours of insulin stimulation (P less than 0.05), especially at insulin treatment for 12 hours (P less than 0.05); Incubated with the selective inhibitor of PI3K (LY294002) and AKT (A-443654), the inhibitory effects of insulin on AQP9 expression decreased (P less than 0.05); but it did not change significantly by blocking the MAPK signaling pathway.;CONCLUSION: ;The insulin treatment inhibited the expression of AQP9 and the PI3K/akt signal transduction pathway was involved in the mechanism.
3.Differential regulation of vascular endothelial growth factor by Akt and mammalian target of rapamycin inhibitors in cell lines derived from childhood solid tumors.
Kurmasheva RT;Harwood FC;Houghton PJ Mol Cancer Ther. 2007 May;6(5):1620-8. Epub 2007 May 4.
Levels of vascular endothelial growth factor (VEGF) are regulated, in part, through activation of the phosphatidylinositol 3'-kinase/Akt pathway. Using pharmacologic inhibitors, we have examined the relative contributions of Akt and mammalian target of rapamycin (mTOR) signaling to VEGF production in neuroblastoma and rhabdomyosarcoma cells growing under normoxic (21% O(2)) or hypoxic (1% O(2)) conditions. Exogenous VEGF stimulated both Akt and extracellular signal-regulated kinase 1/2 phosphorylation in six of seven rhabdomyosarcoma cell lines but in only one of seven neuroblastoma cells, suggesting autocrine stimulation predominantly in rhabdomyosarcoma cell lines. In general, under normoxic conditions, neuroblastoma cells produced more VEGF (120-1,180 pg/10(6) cells/24 h) compared with rhabdomyosarcoma lines (0-200 pg/10(6) cells/24 h). Rapamycin, a selective inhibitor of mTOR, reduced VEGF production in rhabdomyosarcoma cells under normoxic conditions and partially suppressed hypoxia-driven increases in VEGF. However, it poorly inhibited VEGF production under either condition in the majority of neuroblastoma cell lines despite inhibition of mTOR signaling. Rapamycin failed to modulate levels of hypoxia-inducible factor 1alpha (HIF-1alpha) under normoxic conditions and modestly reduced hypoxia-driven increases in HIF-1alpha only in rhabdomyosarcoma cells.
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CAS 552325-16-3 A-443654

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