MOMIPP 是一种PIKfyve抑制剂,是一种巨胞饮作用的诱导剂,可穿过血脑屏障 (BBB)。
产品描述
MOMIPP is a PIKfyve inhibitor and a macropinocytosis inducer. MOMIPP readily penetrates the blood-brain barrier and is moderately effective in suppressing progression of intracerebral glioblastoma xenografts[1][2].
体外活性
MOMIPP can induce intense macropinocytosis, leading to methuosis in cultured glioblastoma cells at low micromolar concentrations[1]. MOMIPP(3 μM) induces cell vacuolization in U373 and Hs683 cell lines[1]. The cytotoxic IPP compound, MOMIPP, causes early disruptions of glucose uptake and glycolytic metabolism. Coincident with these metabolic changes, MOMIPP selectively activates the JNK1/2 stress kinase pathway, resulting in phosphorylation of c-Jun, Bcl-2 and Bcl-xL[2].
体内活性
MOMIPP (80 mg/kg; i.p.; once daily; for 15 consecutive days) shows result that MOMIPP is moderately effective in suppressing progression of intracerebral glioblastoma xenografts.
细胞实验
When JNK activation (phosphorylation) was assessed by western blot analysis after 24 h, MOMIPP(10 μM)has been found that induced major increases in JNK1/2 phosphorylation[2].
动物实验
MOMIPP (Athymic CrTac:NCR-Foxn1 mice (female, 7-8 weeks); 80 mg/kg; i.p.; once daily; for 15 consecutive days) suppressed progression of intracerebral glioblastoma xenografts[2].
Cas No.
1363421-46-8
分子式
C18H16N2O2
分子量
292.33
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years