2. Epigenetics
  3. Histone Methyltransferase
  4. 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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MS2928

MS2928 Chemical Structure

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Based on 1 publication(s) in Google Scholar

MS2928 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

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Description

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[1].

IC50 & Target[1]

SETD8/KMT5A

0.14 μM (IC50)

In Vitro

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.

MS2928 Related Antibodies

Western Blot Analysis[1]

Cell Line: SETD8-overexpressing human multiple myeloma (MM) JJN-3 cells, SETD8-overexpressing human multiple myeloma (MM) OPM-2 cells
Concentration: 2.5 μM, 5.0 μM
Incubation Time: 12 h
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.

Cell Viability Assay[1]

Cell Line: SETD8-overexpressing human multiple myeloma (MM) JJN-3 cells, SETD8-overexpressing human multiple myeloma (MM) OPM-2 cells
Concentration: 1, 1.5, 2, 2.5, 3, 3.5, 4 Log (3 Concentration), nM
Incubation Time: 72 h
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.

Western Blot Analysis[1]

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
Concentration: 0, 0.1, 0.5, 1, 5, 10 μM (MM.1S); 0, 1, 5 μM (KMS20, EJM, PBMC, PNT2, MCF10A)
Incubation Time: 16-24 h
Result: Reduced H4K20me1 levels only at higher concentrations (5 and/or 10 μM) in SETD8-low MM cells and normal cells.

Cell Viability Assay[1]

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
Concentration: 0.06, 0.12, 0.23, 0.47, 0.94, 1.88, 3.75, 7.5, 15 μM
Incubation Time: 72 h
Result: Did not cause significant reduction in cell viability at concentrations up to 15 μM in any of the tested cell lines.
Parmacokinetics
Species Dose Route Cmax Tmax
Mice[1] 15 mg/kg i.p. 10.6 μM 0.25 h
In Vivo

MS2928 (compound 3) (25 mg/kg; i.p.; twice daily; 14 days) significantly inhibits JJN-3 multiple myeloma xenograft tumor growth in female NSG mice with no overt toxicity[1].
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.

Animal Model: NSG (female, 4-5 weeks old, JJN-3 multiple myeloma cell line xenograft)[1]
Dosage: 25 mg/kg
Administration: i.p.; twice daily; 14 days
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.
Animal Model: NSG (female, 4-5 weeks old, OPM-2 multiple myeloma cell line xenograft)[1]
Dosage: 25 mg/kg
Administration: i.p.; twice daily; 16 days
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.
Molecular Weight

412.49

Formula

C21H28N6O3
SMILES

O=C(NCCCNC1=NC(N2CCCC2)=NC3=CC(OCCN)=C(C=C31)OC)C#C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MS2928 Related Classifications

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Help & FAQs
  • 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.

Keywords:

MS2928MS 2928MS-2928Histone MethyltransferaseOPM-2JJN-3H4K20me1NSG miceSETD8xenograft mouse modelsmultiple myeloma cellshistone H4 lysine 20 monomethylationC311SETD8 methyltransferase activityInhibitorinhibitorinhibit

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