雷公藤内酯酮
雷公藤内酯酮 性质
| 熔点 | 251～252℃ |
|---|---|
| 沸点 | 581.1±50.0 °C(Predicted) |
| 密度 | 1.48±0.1 g/cm3(Predicted) |
| 储存条件 | Inert atmosphere,Store in freezer, under -20°C |
| 溶解度 | 二氯甲烷（微溶）、甲醇（微溶） |
| 形态 | 固体 |
| 颜色 | 灰白色至浅米色 |
雷公藤内酯酮 用途与合成方法
| Target | Value |
|
Wnt/β-catenin
() |
Triptonide blocks Wnt/β-catenin signaling via C-terminal transactivation domain of β-catenin, and promots apoptosis in Wnt-dependent cancer cells.
Triptonide potently inhibits the proliferation of human B-lymphoma Raji and T-lymphoma Jurkat cells with IC
50
of 5.7 nM and 4.8 nM, respectively.
Triptonide (2.5-10 nM; 6 days) significantly suppresses B-lymphoma cell colony-forming capability.
Triptonide (20 nM; 3 days) promotes apoptosis through activation of PARP and caspase 3, but reduction of BCL2 protein levels in the lymphoma cells.
Triptonide (5-10 nM; 72 hours) markedly reduces both total and phosphorylated Lyn proteins, and diminishes Lyn downstream ERK and ATK signal pathways.
Cell Proliferation Assay
| Cell Line: | B-lymphoma Raji cells, T-lymphoma Jurkat cells |
| Concentration: | 0-80 nM |
| Incubation Time: | 3 days, 6 days |
| Result: | Inhibited lymphoma cell tumorigenic capability in a dose-dependent manner. |
Apoptosis Analysis
| Cell Line: | Raji cells |
| Concentration: | 5 nM, 10 nM, 20 nM |
| Incubation Time: | 3 days |
| Result: | Did not significantly induce apoptosis at the effective tumor growth-inhibitory (2.5-10 nM); moderately induced lymphoma cell apoptosis (20 nM). |
Western Blot Analysis
| Cell Line: | Raji cells |
| Concentration: | 5 nM, 10 nM, 20 nM |
| Incubation Time: | 3 days |
| Result: | Did not vigorously activated pro-apoptotic proteins PARP and caspase 3 in lymphoma cells (5-10 nM); significantly activated PARP and caspase 3 (20 nM); significantly reduced anti-apoptotic BCL2 levels. |
RT-PCR
| Cell Line: | Raji cells |
| Concentration: | 5 nM, 10 nM |
| Incubation Time: | 72 hours |
| Result: | Significantly diminished Lyn mRNA levels in the lymphoma cells. |
Triptonide (5 mg/kg; i.p.; daily; for 34 days) exerts a strong anti-lymphoma effect in mice.
| Animal Model: | Eight-week-old female NOD/SCID mice (18-22 g), with 3 x 10 7 Raji cells xenograft |
| Dosage: | 5 mg/kg |
| Administration: | Intraperitoneal injection, daily, for 34 days |
| Result: | Potently inhibited lymphoma cell growth and tumorigenic capability. |
药理药效:治疗麻风反应,治疗类风湿性关节炎,治疗肺结核及其他慢性肺部疾病。
雷公藤内酯酮 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-01-25 | HY-32736 | 5 mg | 1278 | ||
| 2024-01-25 | HY-32736 | 雷公藤内酯酮 | 38647-11-9 | 10mg | 2046 |
