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

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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CMP-5 hydrochloride Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CMP-5 hydrochloride Related Antibodies

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.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CMP-5 hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CMP-51030021-40-9CMP5CMP 5Histone MethyltransferaselymphomacellsTh1Th260AEBVPRMT5B-lymphocyteS2Me-H4R3Inhibitorinhibitorinhibit

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