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PP2A Cancerous-IN-1

Names

[ CAS No. ]:
1403933-79-8

[ Name ]:
PP2A Cancerous-IN-1

Biological Activity

[Description]:

PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> PI3K/Akt/mTOR >> Akt

[Target]

pAKT


[In Vitro]

PP2A Cancerous-IN-1 (2.5 and 5 μM; 24 hours; SK-Hep-1 cells) reduces CIP2A expression and cell viability with a dose dependent manner and is more potent in its action than erlotinib[1]. PP2A Cancerous-IN-1 (5 μM; 24 hours; SK-Hep-1 cells) induces cell apoptosis[1]. PP2A Cancerous-IN-1 shows CIP2A inhibitory activity, reduces p-Akt level, induces PARP cleavage. PP2A Cancerous-IN-1 exhibits high potency with low IC50 values of 2.8 μM against HCC cells[1]. Cell Viability Assay[1] Cell Line: SK-Hep-1 cells Concentration: 2.5 and 5 μM Incubation Time: 24 hours Result: Reduced cell viability with a dose dependent manner. Western Blot Analysis[1] Cell Line: SK-Hep-1 cells Concentration: 2.5 and 5 μM Incubation Time: 24 hours Result: Reduced CIP2A expression. Apoptosis Analysis[1] Cell Line: SK-Hep-1 cells Concentration: 2.5 and 5 μM Incubation Time: 24 hours Result: Induced cell apoptosis.

[References]

[1]. Chen KF, et al. Development of erlotinib derivatives as CIP2A-ablating agents independent of EGFR activity. Bioorg Med Chem. 2012;20(20):6144-6153.

Chemical & Physical Properties

[ Molecular Formula ]:
C30H24N4O3

[ Molecular Weight ]:
488.54


Related Compounds