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880813-42-3

中文名称 1-(9-ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine
英文名称 1-(9-ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine
CAS 880813-42-3
分子式 C21H21N3
分子量 315.41
MOL 文件 880813-42-3.mol
更新日期 2024/02/18 21:04:54
880813-42-3 结构式 880813-42-3 结构式

基本信息

中文别名
化合物 T10850
英文别名
CMP5,CMP 5
CMP-5 (PRMT5-IN-5)
1-(9-ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine

物理化学性质

沸点505.1±48.0 °C(Predicted)
密度1.14±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO: 125 mg/mL (396.31 mM)
酸度系数(pKa)7.28±0.20(Predicted)
形态Oil
颜色Light yellow to yellow

常见问题列表

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

IC50: 3.7 μM (mTh1 cells), 9.2 μM (mTh2 cells)IC50: 26.9 μM (hTh1 cells), 31.6 μM (hTh2 cells)

体外研究

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.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.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 IC 50 values are 26.9 μM and 31.6 μM in human Th1 cells and Th2 cells, respectively.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.

Western Blot Analysis

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

Cell Viability Assay

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 increased cell proliferation.
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