1. Epigenetics
  2. Histone Methyltransferase
  3. CMP-5 hydrochloride

CMP-5 hydrochloride 

Cat. No.: HY-113846
Handling Instructions

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.

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CMP-5 hydrochloride Chemical Structure

CMP-5 hydrochloride Chemical Structure

CAS No. : 1030021-40-9

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Description

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]

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].

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.
Molecular Weight

351.87

Formula

C₂₁H₂₂ClN₃

CAS No.

1030021-40-9

SMILES

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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

CMP-5CMP5CMP 5Histone MethyltransferaselymphomacellsTh1Th260AEBVPRMT5B-lymphocyteS2Me-H4R3Inhibitorinhibitorinhibit

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CMP-5 hydrochloride
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