JAS239

JAS239 is a blood-brain barrier-permeable ChoK inhibitor. JAS239 inhibits phosphocholine synthesis and reduces the expression level of E2F1 protein. JAS239 exhibits near-infrared fluorescence properties. JAS239 exerts anti-tumor activity against glioblastoma. JAS239 can be used in studies related to glioblastoma^[1][2][3]. In Vitro:JAS239 (maximum 100 μM; 24 h) reduces the metabolic activity (a surrogate marker for cell viability) of glioblastoma (GBM) cells, and exhibits comparable potency against the F98, 9L, U-87 MG and U-251 MG cell lines under both normoxic and hypoxic conditions^[2].
JAS239 (500 nM; 24-96 h) inhibits the proliferation of GBM cells by inducing cell cycle arrest and downregulating E2F-1 expression^[2].
JAS239 (500 nM; 0-96 h) inhibits the proliferation of the 9L glioblastoma cell line under normoxic conditions^[3]. In Vivo:JAS239 (4 mg/kg; i.p.; once daily; 5 consecutive days) inhibits tumor growth in glioblastoma rats and mice^[1].