LLP-3 是一种有效的Survivin抑制剂，可扰乱癌细胞中的 Survivin-Ran 蛋白复合物作用。LLP-3 可用于多形性胶质母细胞瘤(GBM) 的研究。
| 生物活性 | LLP-3 is a potentSurvivininhibitor that disrupts the Survivin-Ran interaction incancercells. LLP-3 can be used in the research of Glioblastoma multiforme (GBM)[1]. |
| IC50& Target | |
体外研究
(In Vitro) | 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 IC50values 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. |
|
体内研究
(In Vivo) | 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. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
