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880813-42-3

中文名稱 1-(9-ethyl-9H-carbazol-3-yl)-N-(pyridin-2-ylmethyl)methanamine
英文名稱 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 2024/12/25 11:58:24
880813-42-3 結(jié)構(gòu)式 880813-42-3 結(jié)構(gòu)式

基本信息

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

物理化學(xué)性質(zhì)

沸點505.1±48.0 °C(Predicted)
密度1.14±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 125 mg/mL (396.31 mM)
酸度系數(shù)(pKa)7.28±0.20(Predicted)
形態(tài)Oil
顏色Light yellow to yellow

常見問題列表

生物活性
CMP-5 是一種有效的選擇性 PRMT5 抑制劑,對 PRMT1,PRMT4 和 PRMT7 酶無活性。CMP-5 在組蛋白的準(zhǔn)備過程中,通過抑制 PRMT5 甲基轉(zhuǎn)移酶活性選擇性地阻斷 S2Me-H4R3。CMP-5 阻斷 EBV 驅(qū)動的 B 淋巴細(xì)胞轉(zhuǎn)化,但對正常 B 細(xì)胞沒有影響。
靶點

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

體外研究

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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