CMP-5 hydrochloride

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CMP-5 hydrochloride 

CMP-5 hydrochloride 是一种有效的选择性 PRMT5 抑制剂，对 PRMT1，PRMT4 和 PRMT7 酶无活性。CMP-5 hydrochloride 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 hydrochloride 阻断 EBV 驱动的 B 淋巴细胞转化，但对正常 B 细胞没有影响。

CMP-5 hydrochloride

CMP-5 hydrochloride Chemical Structure

CAS No. : 1030021-40-9

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CMP-5 hydrochloride 的其他形式现货产品:

CMP-5

生物活性

CMP-5 hydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 hydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 hydrochloride 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), 36.1 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].
CMP-5 (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].
CMP-5 (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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation 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.

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.

分子量

351.87

Formula

C21H22ClN3
CAS 号

1030021-40-9
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.
参考文献

  • [1]. Alinari L, et al. Selective inhibition of protein arginine methyltransferase 5 blocks initiation and maintenance of B-cell transformation.Blood. 2015 Apr 16;125(16):2530-43.

    [2]. Webb LM, et al. PRMT5-Selective Inhibitors Suppress Inflammatory T Cell Responses and Experimental Autoimmune Encephalomyelitis. J Immunol. 2017 Feb 15;198(4):1439-1451.

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