FNDR-20123

• CAT Number: I045445
• CAS Number: 2641930-61-0
• Molecular Formula: C21H24ClN5O2
• Molecular Weight: 413.90
• Purity: ≥95%
• Synonyms: N-hydroxy-4-[[4-[4-(pyrrolidin-1-ylmethyl)phenyl]triazol-1-yl]methyl]benzamide;hydrochloride
• InChI: InChI=1S/C21H23N5O2.ClH/c27-21(23-28)19-9-5-17(6-10-19)14-26-15-20(22-24-26)18-7-3-16(4-8-18)13-25-11-1-2-12-25;/h3-10,15,28H,1-2,11-14H2,(H,23,27);1H
• InChIKey: UAJSGJVDCCRISR-UHFFFAOYSA-N
• SMILES: C1CCN(C1)CC2=CC=C(C=C2)C3=CN(N=N3)CC4=CC=C(C=C4)C(=O)NO.Cl

FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations[1].
FNDR-20123 is active against all resistant strains tested so far, which will be highly valuable in eliminating the rapidly evolving drug-resistant parasite[1].
FNDR-20123 (10-50 mg/kg; p.o.; bw for 4 days) is also able to reduce parasitaemia significantly in a mouse model for P. falciparum infection[1].

Reference

[1]. Potluri V, et al. Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria. Malar J. 2020;19(1):365. Published 2020 Oct 12.
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