Biochem/physiol Actions

Primary TargetPRMT5

Reversible: yes

Cell permeable: yes

General description

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.

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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

Physical form

Supplied as HCl salt.

Reconstitution

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

Warning

Toxicity: Standard Handling (A)