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Description: LB-100 is a water soluble small-molecular protein phosphatase 2A(PP2A) inhibitor with IC50 of 0.85 uM and 3.87 uM in BxPc-3 and Panc-1 cells. By using CCK-8 assays, LB-100 showed dose-dependent inhibition of cell growth in both cell lines. The IC50 of LB-100 was 0.85 uM and 3.87 uM in BxPc-3 and Panc-1, respectively. While the IC50 of doxorubicin was 2.3 uM and 1.7 uM in BxPc-3 and Panc-1, respectively, LB-100 did not synergize with doxorubicin in both cell lines. LB-100 treatment reduced PP2A activity by 30–50% in different pancreatic cell lines. LB-100 treatment increased the relative concentration of doxorubicin by up to 2.5 fold compared to cells not exposed to LB-100. LB-100 significantly enhanced inhibition of HCC by doxorubicin and cisplatin in vitro and in vivo in a PP2A-dependent way, while having little inhibitory activity when used alone.
References: Cancer Lett. 2014 Dec 28; 355(2):281-7; Mol Cancer Ther. 2014 Aug; 13(8):2062-72.
Related CAS #: 1632032-53-1 1026680-07-8 (deleted)
Chemical Name: 3-[(4-Methylpiperazin-1-yl)carbonyl]-7-oxabicyclo[2.2.1]heptane-2-carboxylic acid
InChi Key: JUQMLSGOTNKJKI-UHFFFAOYSA-N
InChi Code: InChI=1S/C13H20N2O4/c1-14-4-6-15(7-5-14)12(16)10-8-2-3-9(19-8)11(10)13(17)18/h8-11H, 2-7H2, 1H3, (H, 17, 18)
SMILES Code: O=C(C1C(O2)CCC2C1C(N3CCN(C)CC3)=O)O
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