MOPIPP 是一种新型吲哚基查尔酮、液泡素-1，是一种 MOMIPP (HY-148114) 的非致命液泡诱导 2-丙基类似物。MOPIPP 能诱导细胞液泡化，增加自噬体数目。MOPIPP 还会引发细胞巨泡式死亡 (methuosis)，并中断葡萄糖摄取和糖酵解代谢。MOPIPP 能够透过血脑屏障，对胶质母细胞瘤细胞有抑制作用。
| 生物活性 | MOPIPP is a novel indolebased chalcone, and vacuolin-1, is a non-lethal vacuoleinducing 2-propyl analog ofMOMIPP(HY-148114). MOPIPP induces cellular vacuolization and increases autophagosomes numbers. MOPIPP also triggersmethuosis, and interrupts glucose uptake and glycolytic metabolism. MOPIPP can cross the blood-brain barrier and shows efficacy in suppressing tumor progression agaisnt glioblastoma cells[1][2][3]. |
体外研究
(In Vitro) | MOPIPP (10 μM; 48 h) induces cellular vacuolization but does not cause cell death in U251 glioblastoma cells， exhibiting characteristics of late endosomes[1][2].
MOPIPP (10 μM; 24 h) results an increasing LC3 fluorescence associated with the number of autophagosomes and inhibits fusion of autophagosomes with lysosomes[1].
MOPIPP (10 μM; 24 h) increases the amounts of exosomal marker proteins in vesicle fractions recovered from 293T cells[2].
MOMIPP (10 μM; 24 h and 5 h, respectively) causes early disruptions of glucose uptake and glycolytic metabolism, induces methuosis, a form of non-apoptotic cell death, in glioblastoma and other cancer cell lines[3].
MOMIPP (10 μM; 4 h and 24 h) selectively activates the JNK1/2 stress kinase pathway, resulting in phosphorylation of c-Jun, Bcl-2 and Bcl-xL[3].
Immunofluorescence[1] | Cell Line: | U251 glioblastoma cells | | Concentration: | 10 μM | | Incubation Time: | 24 hours; incubated with 2.5 μg/mlAcridine Orange(HY-101879) for 45 min | | Result: | Caused accumulation of autophagosome markers.
Increased punctate LC3 fluorescence and suggested an increase in the number of autophagosomes in cells. |
Western Blot Analysis[3] | Cell Line: | U251 glioblastoma cells | | Concentration: | 10 μM | | Incubation Time: | 4 and 24 hours | | Result: | Triggered increaseing phosphorylation of Bcl-2 and Bcl-xL, accompanied the activation of JNK. |
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体内研究
(In Vivo) | MOMIPP (80 mg/kg; i.p.; single dose) readily penetrates the bloodbrain barrier in female Swiss Webster Mice and (80 mg/kg; i.p.; every 24 h; 15 d) is effective in suppressing progression of intracerebral glioblastoma xenografts in female NCR-Foxn1mice[3].
| Animal Model: | Intracerebral xenograft model in NCR-Foxn1mice (female, 7-8 weeks, injected with U251- LUC cells)[3] | | Dosage: | 80 mg/kg | | Administration: | Intraperitoneal injection; every 24 hours for 15 days; monitored tumor progression by BLI on the days 7, 11, 15 | | Result: | Significantly inhibited tumor progression. |
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| 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. |
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