CMP-5 dihydrochloride
CMP-5 dihydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 dihydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 dihydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected.
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- CAS. Nr.: 2309409-79-6
- Formel: C21H23Cl2N3
- Molecular Weight:388.33
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
IC50: 3.7 μM (mTh1 cells), 9.2 μM (mTh2 cells) 26.9 μM (hTh1 cells), 9.2 μM (hTh2 cells)[1]
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].CMP5 (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].CMP5 (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.
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Cell Line:60A cells
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Concentration:40 μM
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Incubation Time:24 hours
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Result:Inhibited p-BTK and pY(416)SRC protein level.
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Cell Line:Human Th1 cells and Th2 cells
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Concentration:25 μM
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Incubation Time:24 hours
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Result:Inhibited mouse Th1 cell proliferation, but addition of IL-2 dose-dependently increases cell proliferation.
Chemical Information
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CAS. Nr. 2309409-79-6
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Molecular Weight 388.33
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Formel C21H23Cl2N3
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SMILES
CCN1C2=C(C3=C1C=CC=C3)C=C(CNCC4=NC=CC=C4)C=C2.[H]Cl.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Alinari L, et al. Selective inhibition of protein arginine methyltransferase 5 blocks initiation and maintenance of B-cell transformation.Blood. 2015 Apr 16;125(16):2530-43. [Content Brief]
[2]. Webb LM, et al. PRMT5-Selective Inhibitors Suppress Inflammatory T Cell Responses and Experimental Autoimmune Encephalomyelitis. J Immunol. 2017 Feb 15;198(4):1439-1451. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
CMP-5 dihydrochloride Related Classifications
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