1. Epigenetics
  2. Histone Methyltransferase
  3. CMP-5 dihydrochloride

CMP-5 dihydrochloride 是一种有效的选择性 PRMT5 抑制剂,对 PRMT1,PRMT4PRMT7 酶无活性。CMP-5 dihydrochloride 靶向 PRMT5,在组蛋白的准备过程中,通过抑制 PRMT5 甲基转移酶活性选择性地阻断 S2Me-H4R3。CMP-5 dihydrochloride 阻断 EBV 驱动的 B 淋巴细胞转化,但对正常 B 细胞没有影响。

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CMP-5 dihydrochloride Chemical Structure

CMP-5 dihydrochloride Chemical Structure

CAS No. : 2309409-79-6

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CMP-5 dihydrochloride 的其他形式现货产品:

Other Forms of CMP-5 dihydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CMP-5 dihydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 dihydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 dihydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected[1][2].

IC50 & Target

IC50: 3.7 μM (mTh1 cells), 9.2 μM (mTh2 cells)
26.9 μM (hTh1 cells), 9.2 μM (hTh2 cells)[1]

体外研究
(In Vitro)

CMP-5 (0-100 μM; 24-72 hours) is selectively toxic to lymphoma cells, but shows a limited toxicity to normal resting B lymphocytes even after prolonged incubation[1].
CMP-5 (40 μM; 24 hours) decreases p-BTK and pY(416)SRC expression in 60A cells when it compares to the DMSO-treated group[1].
CMP5 (0-40 μM; 24 hours) preferentially suppresses the proliferation of human Th1 cells over Th2 cells (43 versus 9% inhibition, respectively). The sensitivity of Th1 cells over Th2 cells to PRMT5 inhibition is different, the IC50 values are 26.9 μM and 31.6 μM in human Th1 cells and Th2 cells, respectively[1].
CMP5 (25 μM; 24 hours) alone inhibits mouse Th1 cell proliferation by 91%, when added different doses IL-2, IL-2 enhances proliferation and reaches a peak at 5 ng/ml[1].

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

Western Blot Analysis[1]

Cell Line: 60A cells 
Concentration: 40 μM
Incubation Time: 24 hours
Result: Inhibited p-BTK and pY(416)SRC protein level.

Cell Viability Assay[1]

Cell Line: Human Th1 cells and Th2 cells
Concentration: 25 μM
Incubation Time: 24 hours
Result: Inhibited mouse Th1 cell proliferation, but addition of IL-2 dose-dependently increases cell proliferation.
分子量

388.33

Formula

C21H23Cl2N3

CAS 号
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
  • 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.

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产品名称:
CMP-5 dihydrochloride
目录号:
HY-113846A
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