MOMIPP
Names
[ CAS No. ]:
1363421-46-8
[ Name ]:
MOMIPP
[Synonym ]:
trans-3-(5-methoxy-2-methylindol-3-yl)-1-(4-pyridinyl)-2-propen-1-one
Biological Activity
[Description]:
MOMIPP, a macropinocytosis inducer, is a PIKfyve inhibitor. MOMIPP penetrates the blood-brain barrier (BBB)[1][2].
[Related Catalog]:
[In Vitro]
MOMIPP can induce intense macropinocytosis, leading to methuosis in cultured glioblastoma cells at low micromolar concentrations[1]. In U373 and Hs683 cell lines, 3 µM for MOMIPP induces cell vacuolization[1]. MOMIPP (10 μM) causes early disruptions of glucose uptake and glycolytic metabolism. MOMIPP selectively activates the JNK1/2 stress kinase pathway, resulting in phosphorylation of c-Jun, Bcl-2 and Bcl-xL[2]. Western Blot Analysis[2] Cell Line: U251 cells Concentration: 10 μM Incubation Time: 4 h or 24 h Result: Activated the JNK stress kinase pathway.
[In Vivo]
MOMIPP (80 mg/kg; i.p.; once daily; for 15 consecutive days) shows moderately effective in suppressing progression of intracerebral glioblastoma xenografts[2]. Animal Model: Athymic CrTac:NCR-Foxn1 mice (female, 7-8 weeks)[2] Dosage: 80 mg/kg Administration: i.p.; once daily; for 15 consecutive days Result: Suppressed progression of intracerebral glioblastoma xenografts.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C18H16N2O2
[ Molecular Weight ]:
292.33
[ Exact Mass ]:
292.12100
[ PSA ]:
54.98000
[ LogP ]:
3.77600