LB-100 is an inhibitor of protein phosphatase 2A (PP2A) with anticancer activity, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells, respectively[1].
In BxPc-3, Panc-1, and SW1990 cells, LB-100 treatment reduced PP2A activity by 30-50%. LB-100 increases the intracellular doxorubicin concentration (about 2.5 times that of the control group) and makes tumor cells more sensitive to the cytotoxicity of doxorubicin[1].
In a PANC-1 mouse xenograft model, LB-100 (2 mg / kg, intraperitoneal injection) improves the efficacy of the chemotherapy drug doxorubicin. LB-100 increases tumor microvessel density and blood flow velocity on the tumor surface, and decreases tumor volume[1].
Reference:
[1]. Bai X, Zhi X, Zhang Q, et al. Inhibition of protein phosphatase 2A sensitizes pancreatic cancer to chemotherapy by increasing drug perfusion via HIF-1α-VEGF mediated angiogenesis. Cancer Lett, 2014, 355(2): 281-287.