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Biological Activity:

HLCL-61 is a potent and selective Protein arginine methyltransferase-5 (PRMT5) Inhibitor. It shows no inhibitory activity against the type I (PRMT1 and PRMT4) and type II (PRMT7) PRMT family members. HLCL-61 shows effective inhibition of symmetric arginine dimethylation (me2) of histones H3 and H4 in AML samples.Treatment of AML cell lines (MV4-11 and THP-1) and primary blasts with HLCL-61 also results in a decrease of cell viability. HLCL-61 is also effective in promoting apoptosis in MV4-11 and THP-1 cells after 48 h.

How to Use:

In vitro: HLCL-61 was used at 25-50 μM final concentration in various in vitro assays.
In vivo: n/a

Reference:

• 1. Tarighat SS, et al. The dual epigenetic role of PRMT5 in acute myeloid leukemia: gene activation and repression via histone arginine methylation. (2016) Leukemia. 30(4):789-99.?