HLCL-61 is a potent and selective PRMT5 inhibitor for treatment of acute myeloid leukemia. HLCL-61 resulted in significantly increased expression of miR-29b and consequent suppression of Sp1 and FLT3 in AML (acute myeloid leukemia) cells. As a result, significant antileukemic activity was achieved. The increased PRMT5 activity enhanced AML growth in vitro and in vivo while PRMT5 downregulation reduced it. In AML cells, PRMT5 interacted with Sp1 in a transcription repressor complex and silenced miR-29b preferentially via dimethylation of histone 4 arginine residue H4R3.
HLCL-61 hydrochloride is a first-in-class small-molecule inhibitor of PRMT5.
Histone Methyltransferase Inhibitors Related Products:
EPZ005687; GSK343; Tazemetostat; UNC1999; MM-102; SGC0946; SGC2085; OICR-9429; GSK591; SGC707; GSK503; EPZ015666; PFI-2 HCl; UNC0642; UNC0638; GSK-126; EPZ004777; GSK3326595; LLY-507; BRD4770; Pinometostat