Description
FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC 50 s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC 50 =Appearance:SolidIC50& Target:human HDAC 3 nM (IC 50 ) Plasmodium HDAC 31 nM (IC 50 ) HDAC1 25 nM (IC 50 ) HDAC2 29 nM (IC 50 ) HDAC3 2 nM (IC 50 ) HDAC6 11 nM (IC 50 ) HDAC8 282 nM (IC 50 ) PlasmodiumIn Vitro:FNDR-20123 is active against all resistant strains tested so far, which will be highly valuable in eliminating the rapidly evolving drug-resistant parasite. MCE has not independently confirmed the accuracy of these methods. They are for reference onlIn Vivo:FNDR-20123 (10-50mg/kg; p.o.; bw for 4 days) is also able to reduce parasitaemia significantly in a mouse model for P. falciparum infection. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal ModelBiological Activity:FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC 50 s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC 50 =