CMP5 Usage And Synthesis

Description

CMP5 is a potent and selective PRMT5 Inhibitor. CMP5 showed to occupy hPRMT5 catalytic site and block symmetrically dimethylated S2Me-H4R3 & S2Me-H3R8 with no effect on the asymmetric methylation of H4R3 in lymphoblastoid cell lines at 40 μM. CMP-5 shows promise as a novel therapeutic_x000D_ approach for B-cell lymphomas.

Uses

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].

References

[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. DOI:10.1182/blood-2014-12-619783
[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. DOI:10.4049/jimmunol.1601702