CMP-5 hydrochloride

Research use only, not for human use.

CMP-5 (PRMT5-IN-5)is a first-in-class, small-molecule PRMT5-specific inhibitor that blocks EBV-driven B-lymphocyte transformation and survival.

CMP-5 (PRMT5-IN-5)is a first-in-class, small-molecule PRMT5-specific inhibitor that blocks EBV-driven B-lymphocyte transformation and survival, without effect on normal B cells; displays no activity against other type I (PRMT1 and PRMT4) and type II (PRMT7) enzymes; inhibition of PRMT5 leads to lost recruitment of a PRMT5/p65/HDAC3-repressive complex on the miR96 promoter, restored miR96 expression, and PRMT5 downregulation.

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 IC50 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.Cell Proliferation 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 increases cell proliferation. Western Blot Analysis Cell Line:60A cells?Concentration:40 μM Incubation Time:24 hours Result:Inhibited p-BTK and pY(416)SRC protein level.

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PRMT5-IN-5

Chromatin/Epigenetic

HMTase

HMTase

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1030021-40-9

351.87

C21H22ClN3

>98% (HPLC)

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CCN1C2=C(C3=C1C=CC=C3)C=C(CNCC4=NC=CC=C4)C=C2.[H]Cl

1-(9-Ethyl-9H-carbazol-3-yl)-N-(2-pyridinylmethyl)methanamine hydrochloride

(-20℃)

With Ice Pack

≥ 2 years