MEISi-2 is a selective inhibitor of MEIS, a key regulator of hematopoietic stem cell (HSC) self-renewal. MEISi-2 is developed for the research of cardiac injuries, hematopoiesis issues, bone marrow transplantations, and cancer[1].
MEISi-2 does not significantly inhibit the PBX-Luc-reporter[1].MEISi-2 induces MEIS dependent hematopoietic stem cell maintenance and self-renewal[1].MEISi-2 down-regulates MEIS target gene expression[1].MEISi-2 induces murine (LSKCD34low cells) and human (CD34+, CD133+, and ALDHhi cells) HSC self-renewal ex vivo[1].
MEISi-2 (10 µM; i.p.; at day 1, day 4 and day 7) functionally inhibits MEIS in vivo, thus they induces c-Kit+ cell, Sca1+ cell, CD150+ cell, LSK HSPCs, LSKCD34low HSC content and LSKCD150+CD48- HSC content[1].MEISi-2 down-regulates Meis1 expression, Hif-2α, and key CDKI gene expression including p16, p19, p19ARF[1].
[1]. Raife Dilek Turan, et al. Development of Small Molecule MEIS Inhibitors that modulate HSC activity. Sci Rep. 2020; 10: 7994.