LB-100

Uses

LB-100 is a small molecule inhibitor of protein phosphatase 2A with potent chemo- and radio-sensitizing potential in variety of cancer types including pancreatic cancer and colorectal cancer of human and animal model.

Biological Activity

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].[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.