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1-(9-ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine
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- CAS号:
- 880813-42-3
- 英文名:
- 1-(9-ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine
- 英文别名:
- CMP5,CMP 5;CMP-5
(PRMT5-IN-5);9H-Carbazole-3-methanamine, 9-ethyl-N-(2-pyridinylmethyl)-;1-(9-ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine
- 中文名:
- 1-(9-ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine
- 中文别名:
- 化合物 T10850
- CBNumber:
- CB13843906
- 分子式:
- C21H21N3
- 分子量:
- 315.41
- MOL File:
- 880813-42-3.mol
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1-(9-ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine化学性质
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沸点:
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505.1±48.0 °C(Predicted)
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密度:
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1.14±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 125 mg/mL (396.31 mM)
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形态:
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Oil
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酸度系数(pKa):
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7.28±0.20(Predicted)
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颜色:
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Light yellow to yellow
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1-(9-ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine性质、用途与生产工艺
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。
IC50: 3.7 μM (mTh1 cells), 9.2 μM (mTh2 cells)IC50: 26.9 μM (hTh1 cells), 31.6 μM (hTh2 cells)
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
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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
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Cell Line:
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60A cells
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Concentration:
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40 μM
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Incubation Time:
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24 hours
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Result:
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Inhibited p-BTK and pY(416)SRC protein level.
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Cell Viability Assay
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Cell Line:
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Human Th1 cells and Th2 cells
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Concentration:
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25 μM
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Incubation Time:
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24 hours
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Result:
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Inhibited mouse Th1 cell proliferation, but addition of IL-2 dose-dependently increased cell proliferation.
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1-(9-ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine
上下游产品信息
上游原料
下游产品
1-(9-ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine
生产厂家
880813-42-3, 1-(9-ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine 相关搜索:
- 化合物 T10850
- 880813-42-3
- 9H-Carbazole-3-methanamine, 9-ethyl-N-(2-pyridinylmethyl)-
- CMP5,CMP 5
- CMP-5
(PRMT5-IN-5)
- 1-(9-ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine