MS2928
MS2928 is a selective SETD8 inhibitor with an IC50 of 0.14 μM against SETD8 methyltransferase activity. MS2928 reduces cellular H4K20me1 levels and inhibits proliferation of SETD8-overexpressing multiple myeloma cells. MS2928 inhibits tumor growth in xenograft mouse models of SETD8-overexpressing multiple myeloma. MS2928 can be used for the study of SETD8 biological functions and multiple myeloma.
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- Formule: C21H28N6O3
- Masse moléculaire:412.49
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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SETD8/KMT5A 0.14 μM (IC50) |
MS2928 (compound 3) potently inhibits purified human SETD8 methyltransferase activity with an IC50 of 0.14 μM[1].
MS2928 (20 μM; 1 h) covalently modifies wild-type human SETD8 at the C311 residue, as no covalent adduct forms with the SETD8C311S mutant[1].
MS2928 (1 μM) is a selective inhibitor of SETD8, showing no significant inhibition of 20 other human methyltransferases at 1 μM[1].
MS2928 (2.5-5.0 μM; 12 h) reduces H4K20me1 levels in SETD8-overexpressing JJN-3 and OPM-2 human multiple myeloma cells in a concentration-dependent manner after 12 h of treatment[1].
MS2928 (serial dilutions; 72 h) potently inhibits the viability of SETD8-overexpressing JJN-3 and OPM-2 human multiple myeloma cells after 72 h of treatment, with IC50 values of 1.06 μM and 0.54 μM, respectively[1].
MS2928 (0.1-10 μM; 16-24 h) only reduces H4K20me1 levels at higher concentrations in SETD8-low expressing human multiple myeloma cells (MM.1S, KMS20, EJM) and normal human cells (PBMC, PNT2, MCF10A) after 16-24 h of treatment[1].
MS2928 (0.06-15 μM; 72 h) does not significantly inhibit the viability of SETD8-low expressing human multiple myeloma cells (MM.1S, KMS20, EJM) or normal human cells (PBMC, PNT2, MCF10A) at concentrations up to 15 μM after 72 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SETD8-overexpressing human multiple myeloma (MM) JJN-3 cells, SETD8-overexpressing human multiple myeloma (MM) OPM-2 cells
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Concentration:2.5 μM, 5.0 μM
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Incubation Time:12 h
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Result:Reduced H4K20me1 levels in JJN-3 and OPM-2 cells at 2.5 μM.
Achieved near-complete depletion of H4K20me1 in both cell lines at 5.0 μM.
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Cell Line:SETD8-overexpressing human multiple myeloma (MM) JJN-3 cells, SETD8-overexpressing human multiple myeloma (MM) OPM-2 cells
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Concentration:1, 1.5, 2, 2.5, 3, 3.5, 4 Log (3 Concentration), nM
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Incubation Time:72 h
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Result:Inhibited JJN-3 cell viability with an IC50 of 1.06 μM.
Inhibited OPM-2 cell viability with an IC50 of 0.54 μM.
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Cell Line:SETD8-low expressing human multiple myeloma (MM) MM.1S cells, SETD8-low expressing human multiple myeloma (MM) KMS20 cells, SETD8-low expressing human multiple myeloma (MM) EJM cells, normal human PBMC cells, normal human PNT2 cells, normal human MCF10A cells
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Concentration:0, 0.1, 0.5, 1, 5, 10 μM (MM.1S); 0, 1, 5 μM (KMS20, EJM, PBMC, PNT2, MCF10A)
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Incubation Time:16-24 h
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Result:Reduced H4K20me1 levels only at higher concentrations (5 and/or 10 μM) in SETD8-low MM cells and normal cells.
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Cell Line:SETD8-low expressing human multiple myeloma (MM) MM.1S cells, SETD8-low expressing human multiple myeloma (MM) KMS20 cells, SETD8-low expressing human multiple myeloma (MM) EJM cells, normal human PBMC cells, normal human PNT2 cells, normal human MCF10A cells
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Concentration:0.06, 0.12, 0.23, 0.47, 0.94, 1.88, 3.75, 7.5, 15 μM
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Incubation Time:72 h
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Result:Did not cause significant reduction in cell viability at concentrations up to 15 μM in any of the tested cell lines.
| Species | Dose | Route | Cmax | Tmax |
|---|---|---|---|---|
| Mice[1] | 15 mg/kg | i.p. | 10.6 μM | 0.25 h |
MS2928 (25 mg/kg; i.p.; twice daily; 16 days) significantly inhibits OPM-2 multiple myeloma xenograft tumor growth in female NSG mice, reduces tumor cell proliferation and SETD8-mediated H4K20 monomethylation, and is well tolerated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG (female, 4-5 weeks old, JJN-3 multiple myeloma cell line xenograft)[1]
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Dosage:25 mg/kg
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Administration:i.p.; twice daily; 14 days
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Result:Significantly reduced tumor growth relative to controls, with statistical significance noted at days 8, 10, 12, and 14 of treatment.
Caused no significant body weight loss or overt toxicity.
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Animal Model:NSG (female, 4-5 weeks old, OPM-2 multiple myeloma cell line xenograft)[1]
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Dosage:25 mg/kg
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Administration:i.p.; twice daily; 16 days
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Result:Significantly reduced tumor growth relative to controls, with statistical significance noted from day 4 through day 16 of treatment.
Caused only slight, non-significant body weight loss.
Markedly reduced Ki-67 (proliferation marker) and H4K20me1 (SETD8 activity marker) staining in tumor tissues relative to controls.
Chemical Information
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Masse moléculaire 412.49
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Formule C21H28N6O3
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SMILES
O=C(NCCCNC1=NC(N2CCCC2)=NC3=CC(OCCN)=C(C=C31)OC)C#C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MS2928 Related Classifications
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