2. Epigenetics
  3. Histone Methyltransferase
  4. MS2928

MS2928 是一种选择性 SETD8 抑制剂，对 SETD8 甲基转移酶活性的 IC50 为 0.14 μM。MS2928 可降低细胞内 H4K20me1 水平，并抑制过表达 SETD8 的多发性骨髓瘤细胞增殖。MS2928 可在过表达 SETD8 的多发性骨髓瘤异种移植小鼠模型中抑制肿瘤生长。MS2928 可用于 SETD8 生物学功能及多发性骨髓瘤的研究。

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MS2928

MS2928 Chemical Structure

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MS2928 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

MS2928 (compound 3) 可强效抑制纯化的人源 SETD8 甲基转移酶活性，其 IC50 为 0.14 μM[1]。
MS2928 (20 μM; 1 h) 可共价修饰野生型人源 SETD8 的 C311 位点，因为其无法与 SETD8C311S 突变体形成共价加合物[1]。
MS2928 (1 μM) 是 SETD8 的选择性抑制剂，在 1 μM 浓度下对其他 20 种人类甲基转移酶无显著抑制作用[1]。
MS2928 (2.5-5.0 μM; 12 h) 可在处理 12 h 后以浓度依赖的方式降低过表达 SETD8 的人多发性骨髓瘤 JJN-3 和 OPM-2 细胞中的 H4K20me1 水平[1]。
MS2928 (72 h) 可强效抑制过表达 SETD8 的人多发性骨髓瘤细胞系 JJN-3 和 OPM-2 的细胞活力，处理 72 h 后，其 IC50 值分别为 1.06 μM 和 0.54 μM[1]。
MS2928 (0.1-10 μM; 16-24 h) 仅在较高浓度下，于处理 16-24 h 后低表达 SETD8 的人多发性骨髓瘤细胞 (MM.1S、KMS20、EJM) 和正常人细胞 (PBMC、PNT2、MCF10A) 中的 H4K20me1 水平[1]。
MS2928 (0.06-15 μM; 72 h) 在处理 72 h 后，浓度高达 15 μM 时也不会显著抑制低表达 SETD8 的人多发性骨髓瘤细胞 (MM.1S、KMS20、EJM) 或正常人细胞 (PBMC、PNT2、MCF10A) 的活力[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MS2928 相关抗体:

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.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax Tmax
Mice[1] 15 mg/kg i.p. 10.6 μM 0.25 h
体内研究
(In Vivo)

MS2928 (compound 3) (腹腔注射，25 mg/kg，每日 2 次，连续 14 天) 可显著抑制雌性 NSG 小鼠体内 JJN-3 多发性骨髓瘤异种移植瘤的生长，且无明显毒性[1]。
MS2928 (腹腔注射；25 mg/kg；每日 2 次；连续 16 天) 可显著抑制雌性 NSG 小鼠体内 OPM-2 多发性骨髓瘤异种移植瘤的生长，降低肿瘤细胞增殖水平及 SETD8 介导的 H4K20 单甲基化修饰，且具有良好的耐受性[1]。

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.
分子量

412.49

Formula

C21H28N6O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MS2928 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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目录号：
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