JX21108

JX21108 (200 nM; 72 h) exhibits potent in vitro antiplasmodial activity against both drug-sensitive (3D7) and multidrug-resistant (Dd2) P. falciparum strains^[1].
JX21108 (200 nM; 72 h) has potent in vitro activity against diverse multidrug-resistant P. falciparum strains^[1].
JX21108 (700 nM; 6 h) is highly effective against ring-stage P. falciparum parasites^[1].
JX21108 (10 μM; 48 h) exhibits potent gametocytocidal activity against both stage II and stage IV P. falciparum gametocytes^[1].
JX21108 (40 nM; 12 h) inhibits P. falciparum blood-stage development, with the schizont stage being the most sensitive to its parasiticidal effects^[1].
JX21108 (10-100 nM; 3-24 h) has potent, time- and dose-dependent antiplasmodial activity against P. falciparum 3D7, with a short exposure at a high concentration sufficient to completely block parasite growth^[1].
JX21108 (5-20 nM; 4 h) acts as a histone deacetylase (HDAC) inhibitor in P. falciparum, leading to increased histone H3 acetylation^[1].
The docking study suggests that (R)-JX21108 has a strong binding affinity for the PfHDAC1 active site, primarily through interactions with the Zn²⁺ ion and surrounding residues^[1].
JX21108 treatment causes broadly similar transcriptomic changes to PfHDAC1 knockdown in P. falciparum, particularly the downregulation of genes involved in host cell invasion, further validating PfHDAC1 as the target^[1].
JX21108 is a potent in vitro antiplasmodial compound against P. falciparum 3D7 (EC₅₀ = 3.6 nM) and Dd2 (EC₅₀ = 4.0 nM)^[2].

JX21108 (100 μM; 72 h) has a favorable safety profile in vitro, with high selectivity indices against HepG2 and 293T cells^[1].
JX21108 (1.5 µM; 0-45 min) exhibits high metabolic stability in mouse and human liver microsomes but is rapidly metabolized in rat liver microsomes^[1].