LLP3

LLP-3 is a potent Survivin inhibitor that disrupts the Survivin-Ran interaction in cancer cells. LLP-3 can be used in the research of Glioblastoma multiforme (GBM)[1].

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> Survivin

Survivin[1]

LLP-3 (20 μM, 24 h) impaires the binding of Survivin to Smac/DIABLO (proapoptotic protein), without affecting the interaction of Survivin with other chromosomal passenger complex (CPC) proteins[1]. LLP-3 (20 μM, 24 h) decreases the Survivin-Ran interaction in U87 cells[1]. LLP-3 (20 μM, 24 h) arrests cell in G0-G1 phase and subsequent tumor cell death[1]. LLP-3 (20 μM, 24 h) triggers caspase-dependent apoptosis in HT1080 cells[1]. LLP-3 (0-100 μM, 72 h) inhibits tumor cells survival by p53-mediated inhibition[1]. Cell Viability Assay[1] Cell Line: U87E6, U87MG cell Concentration: 0-100 μM Incubation Time: 72 h Result: Inhibited tumor cells survival with IC50 values of 13.6 μM (U87E6) and 38.1 μM (U87MG). Cell Cycle Analysis[1] Cell Line: U87 cells Concentration: 20 μM Incubation Time: 24 h Result: Reduced the proportions of cells in the S and G2-M phases (from 9% to 5%, and from 25% to 17%, respectively). Increased G0-G1 cell population (from 60% to 74%). Immunofluorescence[1] Cell Line: U87, HT1080 cells Concentration: 40 μM Incubation Time: 24 h Result: Weakened the colocalization of TPX2 with the acetylated α-tubulin.

LLP-3 (intraperitoneal injection, 25 mg/kg, for 10 days) prolongs survival of GBM sphere-derived tumor mice[1]. Animal Model: GBM sphere-derived tumor models (GBM83 and 1600)[1] Dosage: 25 mg/kg Administration: Intraperitoneal injection, for 10 days (days 10–14 and days 17–21) Result: Prolonged the survival of tumor-burden mice without exhibiting any lethality of mice until day 35.

[1]. Hacer Guvenc, et al. Impairment of glioma stem cell survival and growth by a novel inhibitor for Survivin-Ran protein complex. Clin Cancer Res. 2013 Feb 1;19(3):631-42.