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CMP-5 hydrochloride

Catalog No. T19243   CAS 1030021-40-9

CMP-5 hydrochloride is a potent and selective PRMT5 inhibitor, while displays no activity against PRMT1/4/7 enzymes. It selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations.

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CMP-5 hydrochloride Chemical Structure
CMP-5 hydrochloride, CAS 1030021-40-9
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,520.00
50 mg 6-8 weeks $ 1,980.00
100 mg 6-8 weeks $ 2,500.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CMP-5 hydrochloride is a potent and selective PRMT5 inhibitor, while displays no activity against PRMT1/4/7 enzymes. It selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations.
Targets&IC50 hTh1 cells:26.9 μM , hTh2 cells:36.1 μM , MTH1 (cells):3.7 μM , MTH2 (cells):9.2 μM
In vitro CMP-5 (0-100 μM; 24-72 hours) is selectively toxic to lymphoma cells but shows limited toxicity to normal resting B lymphocytes even after prolonged incubation. 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 (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 (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].
Molecular Weight 351.87
Formula C21H22ClN3
CAS No. 1030021-40-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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. 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.

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Keywords

CMP-5 hydrochloride 1030021-40-9 Others CMP 5 hydrochloride CMP 5 Hydrochloride CMP-5 Hydrochloride CMP5 Hydrochloride CMP5 hydrochloride inhibitor inhibit

 

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