1. Autophagy
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  3. MOPIPP

MOPIPP is a novel indolebased chalcone, and vacuolin-1, is a non-lethal vacuoleinducing 2-propyl analog of MOMIPP (HY-119624). MOPIPP induces cellular vacuolization and increases autophagosomes numbers. MOPIPP also triggers methuosis, and interrupts glucose uptake and glycolytic metabolism. MOPIPP can cross the blood-brain barrier and shows efficacy in suppressing tumor progression agaisnt glioblastoma cells.

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MOPIPP

MOPIPP Chemical Structure

CAS No. : 1485521-76-3

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Based on 1 publication(s) in Google Scholar

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Description

MOPIPP is a novel indolebased chalcone, and vacuolin-1, is a non-lethal vacuoleinducing 2-propyl analog of MOMIPP (HY-119624). MOPIPP induces cellular vacuolization and increases autophagosomes numbers. MOPIPP also triggers methuosis, 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].

Cellular Effect
Cell Line Type Value Description References
U-251 GI50
15.3 μM
Compound: 19
Growth inhibition of human U251 cells preincubated for 24 hrs followed by compound-washout measured at 48 hrs by sulforhodamine assay
Growth inhibition of human U251 cells preincubated for 24 hrs followed by compound-washout measured at 48 hrs by sulforhodamine assay
[PMID: 24527179]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Immunofluorescence[1]

Cell Line: U251 glioblastoma cells
Concentration: 10 μM
Incubation Time: 24 hours; incubated with 2.5 μg/ml Acridine 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.
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-Foxn1 mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Intracerebral xenograft model in NCR-Foxn1 mice (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.
Molecular Weight

320.39

Formula

C20H20N2O2

CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

O=C(C1=CC=NC=C1)/C=C/C(C2=C3)=C(CCC)NC2=CC=C3OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 8.33 mg/mL (26.00 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1212 mL 15.6060 mL 31.2120 mL
5 mM 0.6242 mL 3.1212 mL 6.2424 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1212 mL 15.6060 mL 31.2120 mL 78.0299 mL
5 mM 0.6242 mL 3.1212 mL 6.2424 mL 15.6060 mL
10 mM 0.3121 mL 1.5606 mL 3.1212 mL 7.8030 mL
15 mM 0.2081 mL 1.0404 mL 2.0808 mL 5.2020 mL
20 mM 0.1561 mL 0.7803 mL 1.5606 mL 3.9015 mL
25 mM 0.1248 mL 0.6242 mL 1.2485 mL 3.1212 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
MOPIPP
Cat. No.:
HY-148114
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