LLC0424 N is a negative control compound designed by methylating the thalidomide moiety of LLC0424. LLC0424 N shows does not induce NSD2 degradation and inhibit growth of acute lymphoblastic leukemia cells with NSD2 mutation. LLC0424 N can be used for the research of acute lymphoblastic leukemia [1].
In Vitro, LLC0424N (0.5-2 μM; 12-24 h) does not potently degrade NSD2 protein in SEM ALL cells[1]. LLC0424N (2 μM; 8-24 h) does not downregulate NSD2 or H3K36me2 protein levels in SEM ALL and RPMI-8402 cells[1]. LLC0424N (100 nM-30 μM; 7 days) does not dose-dependently inhibit the growth of SEM ALL and RPMI-8402 cells[1]. LLC0424N (2 μM; 30 days ) does not reduce colony formation or size in RPMI-8402 ALL cells[1].
References:
[1]. Liu L, et al. Discovery of LLC0424 as a Potent and Selective in Vivo NSD2 PROTAC Degrader[J]. Journal of Medicinal Chemistry, 2024, 67(9): 6938-6951.
In Vitro, LLC0424N (0.5-2 μM; 12-24 h) does not potently degrade NSD2 protein in SEM ALL cells[1]. LLC0424N (2 μM; 8-24 h) does not downregulate NSD2 or H3K36me2 protein levels in SEM ALL and RPMI-8402 cells[1]. LLC0424N (100 nM-30 μM; 7 days) does not dose-dependently inhibit the growth of SEM ALL and RPMI-8402 cells[1]. LLC0424N (2 μM; 30 days ) does not reduce colony formation or size in RPMI-8402 ALL cells[1].
References:
[1]. Liu L, et al. Discovery of LLC0424 as a Potent and Selective in Vivo NSD2 PROTAC Degrader[J]. Journal of Medicinal Chemistry, 2024, 67(9): 6938-6951.