PRMT5 Inhibitor, CMP5

A cell-permeable carbazole based compound that selectively inhibits PRMT5 and not PRMT1, PRMT4 & PRMT7 activity. Shown 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. Prevents Epstein-Barr virus (EBV)-driven B cell immortalization and restores miR-96 transcriptional activity. Dose-dependently induces lymphoma cell death over normal resting B lymphocytes.

A cell-permeable carbazole based compound that selectively inhibits PRMT5 and not PRMT1, PRMT4 & PRMT7 activity. Shown 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. Prevents Epstein-Barr virus (EBV)-driven B cell immortalization and restores miR-96 transcriptional activity. Dose-dependently induces lymphoma cell death over normal resting B lymphocytes.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Cell permeable: yes

Primary Target
PRMT5

Reversible: yes

Packaged under inert gas

Toxicity: Standard Handling (A)

Supplied as HCl salt.

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Alinari, L., et al. 2015. Blood.125, 2530.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany