MS910
MS910 is a CRBN-recruiting MEK1/2 PROTAC degrader, with a DC50 of 94 nM against MEK1 and 38 nM against MEK2 in SK-MEL-28 cells. MS910 induces the degradation of GSPT1, IKZF1/3 and ZFP91, thereby inhibiting the downstream ERK signaling pathway and cancer cell growth. MS910 is applicable to research related to colorectal cancer and melanoma.
(Pink: MEK1 and MEK2 ligand (HY-10254); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-W022240)).
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- CAS. Nr.: 2756323-28-9
- Formel: C41H48F3IN6O11
- Molecular Weight:984.75
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
MEK1 94 nM (DC50, SK-MEL-28 cells) |
MEK2 38 nM (DC50, SK-MEL-28 cells) |
MEK1 118 nM (DC50, HT-29 cells) |
MEK2 55 nM (DC50, HT-29 cells) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HT-29 | GI50 |
0.3 μM
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Antiproliferative activity against human HT-29 colorectal cancer cells assessed as reduction in cell viability incubated for 3 days by WST-8 assay.
Antiproliferative activity against human HT-29 colorectal cancer cells assessed as reduction in cell viability incubated for 3 days by WST-8 assay.
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33284613 |
| SK-MEL-28 | GI50 |
780 nM
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Antiproliferative activity against human SK-MEL-28 melanoma cells assessed as reduction in cell viability incubated for 3 days by WST-8 assay.
Antiproliferative activity against human SK-MEL-28 melanoma cells assessed as reduction in cell viability incubated for 3 days by WST-8 assay.
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33284613 |
| HT-29 | DC50 |
118 nM
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Degradation of MEK1 in human HT-29 colorectal cancer cells incubated for 24 h measured by Western blot assay.
Degradation of MEK1 in human HT-29 colorectal cancer cells incubated for 24 h measured by Western blot assay.
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33284613 |
| HT-29 | DC50 |
55 nM
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Degradation of MEK2 in human HT-29 colorectal cancer cells incubated for 24 h measured by Western blot assay.
Degradation of MEK2 in human HT-29 colorectal cancer cells incubated for 24 h measured by Western blot assay.
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33284613 |
| SK-MEL-28 | DC50 |
94 nM
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Degradation of MEK1 in human SK-MEL-28 melanoma cells incubated for 24 h measured by Western blot assay.
Degradation of MEK1 in human SK-MEL-28 melanoma cells incubated for 24 h measured by Western blot assay.
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33284613 |
| SK-MEL-28 | DC50 |
38 nM
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Degradation of MEK2 in human SK-MEL-28 melanoma cells incubated for 24 h measured by Western blot assay.
Degradation of MEK2 in human SK-MEL-28 melanoma cells incubated for 24 h measured by Western blot assay.
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33284613 |
In Vitro
MS910 (compound 50) (3 days) inhibits the proliferation of SK-MEL-28 melanoma cells, with a GI50 of 780 nM[1].
MS910 (3 days) potently inhibits the proliferation of HT-29 colorectal cancer cells, with a GI50 of 0.3 μM[1].
MS910 (0-10 μM; 24 h) potently and selectively degrades MEK1 (DC50 = 118 nM) and MEK2 (DC50 = 55 nM) in HT-29 cells, while inhibiting the phosphorylation of downstream MEK and ERK[1].
MS910 (0-10 μM; 24 h) efficiently and selectively degrades MEK1 (DC50 = 94 nM) and MEK2 (DC50 = 38 nM) in SK-MEL-28 cells, while inhibiting the phosphorylation of downstream MEK and ERK[1].
MS910 (0.3 μM; 2-24 h) induces time-dependent degradation of MEK1 and MEK2 in HT-29 cells, with significant degradation observed at 4 h, maximal degradation achieved at 8-10 h, followed by inhibition of ERK phosphorylation[1].
MS910 (0.3 μM; 8 h) induces the degradation of MEK1/2 in HT-29 cells via the ubiquitin-proteasome system in a CRBN-dependent manner, a process that requires binding to MEK1/2[1].
MS910 (0-300 nM; 10 days) effectively inhibits colony formation of HT-29 colorectal cancer cells, and exhibits stronger activity than its non-degradative control[1].
Treatment of HT-29 and SK-MEL-28 cells with MS910 (0.1 nM-10 μM) for 24 h induces concentration-dependent degradation of MEK1 and MEK2 proteins[1].
MS910 (1 nM-100 μM) binds to MEK1 and MEK2 proteins in a concentration-dependent manner[1].
Treatment of HT-29 cells with MS910 (0.3 μM; 8 h) reduces the protein levels of MEK1 and MEK2[1].
MS910 (0.0001-10 μM; 24 h) induces concentration-dependent degradation of MEK1, MEK2, GSPT1, IKZF1 and IKZF3, but does not induce ZFP91 degradation, following 24-hour treatment of HT-29 cells[1].
MS910 (0.3 μM; 8 h) exhibits high selectivity for MEK1 and MEK2 in HT-29 cells[1].
MS910 (0.0001-10 μM; 24 h) does not degrade most CRBN neo-substrates (GSPT1, IKZF1, ZFP91) in HT-29 cells, but degrades IKZF3 at concentrations above 1 μM, and exhibits higher potency in degrading MEK1/2 than IKZF3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-29 cells
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Concentration:0.3 μM
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Incubation Time:8 h
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Result:Reduced MEK1 and MEK2 protein levels relative to DMSO control, confirming degradation of these proteins.
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Cell Line:HT-29 cells
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Concentration:0.0001, 0.0003, 0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
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Incubation Time:24 h
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Result:Induced concentration-dependent degradation of MEK1 and MEK2 proteins.
Reduced GSPT1, IKZF1, and IKZF3 protein levels in a concentration-dependent manner.
Left ZFP91 protein levels unchanged across all tested concentrations.
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Cell Line:HT-29 colorectal cancer cells
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Concentration:0.0001, 0.0003, 0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
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Incubation Time:24 h
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Result:Degraded MEK1 with a DC50 of 118 nM in a concentration-dependent manner.
Degraded MEK2 with a DC50 of 55 nM in a concentration-dependent manner.
Inhibited phosphorylation of MEK and ERK in a concentration-dependent manner.
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Cell Line:SK-MEL-28 melanoma cells
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Concentration:0.0001, 0.0003, 0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
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Incubation Time:24 h
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Result:Degraded MEK1 with a DC50 of 94 nM in a concentration-dependent manner.
Degraded MEK2 with a DC50 of 38 nM in a concentration-dependent manner.
Inhibited phosphorylation of MEK and ERK in a concentration-dependent manner.
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Cell Line:HT-29 colorectal cancer cells
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Concentration:0.3 μM
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Incubation Time:0-24 h
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Result:Induced significant MEK1/2 degradation starting at 4 h.
Reached maximum MEK1/2 degradation within 8-10 h.
Inhibited ERK phosphorylation starting at 8-10 h.
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Cell Line:HT-29 colorectal cancer cells
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Concentration:0.3 μM
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Incubation Time:8 h
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Result:Blocked MEK1/2 degradation induced by MS910 via pretreatment with PD0325901, MG-132, MLN4924, and pomalidomide.
Restored pMEK and pERK levels via pretreatment with PD0325901, MG-132, MLN4924, and pomalidomide.
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Cell Line:HT-29 colorectal cancer cells
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Concentration:0.0001, 0.0003, 0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM
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Incubation Time:24 h
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Result:Did not significantly reduce GSPT1, IKZF1, or ZFP91 protein levels at concentrations up to 10 μM.
Significantly decreased IKZF3 protein levels at concentrations above 1 μM, with lower potency for IKZF3 degradation compared to MEK1/2.
Chemical Information
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CAS. Nr. 2756323-28-9
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Molecular Weight 984.75
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Formel C41H48F3IN6O11
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SMILES
O=C(C1=CC=C(C(F)=C1NC2=CC=C(C=C2F)I)F)NOCCCNCCOCCOCCOCCOCCOCCNC3=CC=C4C(N(C5C(NC(CC5)=O)=O)C(C4=C3)=O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MS910 Related Classifications
HY-170982 Related Classifications
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