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Cat. No.: HY-181849

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MS2928

Name: MS2928
Brand: MedChemExpress
SKU: HY-181849
Price: 925.00 USD
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MS2928 is a selective SETD8 inhibitor with an IC₅₀ of 0.14 μM against SETD8 methyltransferase activity. MS2928 reduces cellular H4K20_me1 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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화학식: C₂₁H₂₈N₆O₃
분자량:412.49

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

MS2928 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

SETD8/KMT5A

0.14 μM (IC₅₀)

All Histone Methyltransferase Isoforms :

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 SETD8^C311S 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 H4K20_me1 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 H4K20_me1 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.

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	C_max	T_max
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.

Chemical Information

분자량 412.49
화학식 C₂₁H₂₈N₆O₃
SMILES

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

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Chen H, et al. Discovery of a Potent, Selective, and In Vivo Efficacious Covalent Inhibitor for Lysine Methyltransferase SETD8. J Med Chem. 2026;69(4):4255-4269. [Content Brief]

Calculators

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Mass Mass

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Molecular Weight Molecular Weight

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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MOQ

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100 mg

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

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MS2928

All Histone Methyltransferase Isoforms