MG-Lin1
MG-Lin1 is a Lin28/Lin28A molecular glue degrader with a DC50 of approximately 0.7 μM. It induces Lin28 degradation via the ubiquitin-proteasome pathway by forming a ternary complex, thereby upregulating the levels of let-7 miRNA and reducing the expression of its downstream oncogenic targets KRAS and PDK1, and inhibiting cancer cell migration. MG-Lin1 can be used in studies of ovarian cancer and choriocarcinoma.
For research use only. We do not sell to patients.
- Formula: C23H18F3N5O
- Molecular Weight:437.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
Lin28 0.7 μM (DC50) |
Ras |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PA-1 | EC50 |
0.1 μM
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50% reduction of normalized Renilla luciferase intensity in human PA-1 ovarian cancer cells via Lin28/let-7 luciferase reporter assay following 24 h incubation.
50% reduction of normalized Renilla luciferase intensity in human PA-1 ovarian cancer cells via Lin28/let-7 luciferase reporter assay following 24 h incubation.
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39575661 |
| PA-1 | DC50 |
0.7 μM
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Proteasome-dependent degradation of endogenous Lin28 protein in human PA-1 ovarian cancer cells measured via western blot following 48 h incubation.
Proteasome-dependent degradation of endogenous Lin28 protein in human PA-1 ovarian cancer cells measured via western blot following 48 h incubation.
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39575661 |
In Vitro
MG-Lin1 (0.1-100 μM; 24 h) potently enhances the activity of let-7 in PA-1 ovarian cancer cells, reducing the normalized luciferase intensity by 50% after 24 h of incubation at a concentration of 0.1 μM[1].
MG-Lin1 (0.01-10 μM; 48 h) induces proteasome-dependent degradation of Lin28 in PA-1 ovarian cancer cells, with a degradation rate of 66% after treatment at 1 μM for 48 h, and its DC50 is approximately 0.7 μM[1].
MG-Lin1 (1-10 μM; 48 h) significantly increases the abundance of let-7c miRNA in PA-1 ovarian cancer cells, with the abundance elevated by more than 2-fold after treatment at 10 μM for 48 h[1].
MG-Lin1 (10 μM; 48 h) reduces the mRNA levels of oncogenic KRAS and PDK1 in PA-1 ovarian cancer cells; after incubation at 10 μM for 48 h, the level of KRAS decreases to approximately 60% of that in the vehicle control group, and the level of PDK1 decreases to approximately 35% of that in the vehicle control group[1].
MG-Lin1 (10 μM; 72 h) reduces the migration capacity of PA-1 ovarian cancer cells by 55% after incubation at a concentration of 10 μM for 72 h[1].
MG-Lin1 (10 μM; 48 h) more effectively increases the abundance of let7-c in JAR cells compared with other tested degraders[1].
MG-Lin1 (1 μM; 24 h) reduces the mRNA expression levels of KRAS and PDK1 in PA1 cells[1].
MG-Lin1 (48 h) reduces the KRAS protein level in JAR cells to 66% of that in the vehicle control group[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PA-1 ovarian cancer cells
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Concentration:0.01, 0.1, 1, 10 μM; 10 μM (with proteasome inhibitor co-treatment)
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Incubation Time:48 h
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Result:Reduced Lin28 protein levels in a dose-dependent manner, causing a 66% decrease at 1 μM, with a DC50 of approximately 0.7 μM.
Blocked Lin28 reduction when co-treated with proteasome inhibitors, confirming proteasome-mediated degradation.
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Cell Line:PA-1 ovarian cancer cells
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Concentration:1, 10 μM
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Incubation Time:48 h
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Result:Increased relative let-7c abundance significantly, with a greater than 2-fold increase observed at 10 μM.
Showed a more pronounced increase than a comparable PROTAC derivative at the same dose.
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Cell Line:PA-1 ovarian cancer cells
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Concentration:10 μM
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Incubation Time:48 h
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Result:Reduced relative KRAS mRNA abundance significantly to approximately 60% of vehicle control.
Reduced relative PDK1 mRNA abundance significantly to approximately 35% of vehicle control.
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Cell Line:PA-1 ovarian cancer cells
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Concentration:10 μM
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Incubation Time:72 h
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Result:Inhibited PA-1 cell migration significantly, reducing wound closure by 55% as measured by relative wound density compared to untreated cells.
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Cell Line:JAR cells
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Concentration:10 μM
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Incubation Time:48 h
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Result:Increased let7-c abundance to a level higher than vehicle control.
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Cell Line:PA1 cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Decreased KRAS mRNA levels relative to vehicle control.\nDecreased PDK1 mRNA levels relative to vehicle control.
Chemical Information
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Molecular Weight 437.42
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Formula C23H18F3N5O
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SMILES
CC1=NN=C2C=CC(C3=CC=CC(N(C)C(/C=C/C4=CC=C(C=C4)C(F)(F)F)=O)=C3)=NN12
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)