LSPN954 

LSPN954 (compound 4i) is an indole-based peptidomimetic antiplasmodial agent that exhibits submicromolar activity against both sensitive and multidrug-resistant *Plasmodium falciparum* strains, with low cytotoxicity to human cells and a high selectivity index. LSPN954 shows slow-acting inhibitory activity, allowing the initial development of *Plasmodium* followed by morphological changes, and its activity is independent of the inhibition of plastid-dependent isoprenoid biosynthesis. LSPN954 can be used in malaria research^[1].

LSPN954 (compound 4i) (0.049-50 μM; 72 h for P. falciparum; 1.56-100 μM; 72 h for HepG2) potently inhibits Plasmodium falciparum 3D7 growth with an IC₅₀ of 1.7 μM, shows low cytotoxicity against human HepG2 and HEK293 cells, and has high selectivity indices of 59 and >59, respectively^[1].
LSPN954 (0.049-50 μM; 24, 48, 72 h exposure periods; 10× IC₅₀; 24 h morphological analysis) exhibits slow-acting inhibitory activity against Plasmodium falciparum 3D7, as shown by IC₅₀ ratios above 1 for 24 h vs 72 h exposure and a 4-fold ratio for 6-day vs 4-day regrowth, plus morphological evidence of parasite recovery after initial exposure^[1].
LSPN954 (0.01-100 μM; 72 h, with 200 μM IPP co-treatment) antiplasmodial activity against Plasmodium falciparum 3D7 is not reversed by IPP supplementation, indicating its activity does not involve inhibition of apicoplast-dependent isoprenoid biosynthesis^[1].
LSPN954 (0.049-50 μM; 72 h) retains potent antiplasmodial activity against multidrug-resistant Plasmodium falciparum strains (3D7R_MMV848, Dd2R_DSM265, Dd2, K1, TM90C6B) with resistance indices close to 1, indicating no cross-resistance with standard antimalarials^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

564.72

C₃₅H₄₀N₄O₃

CC1=CC=C(C=C1)C(C2=CC3=CC=CC=C3N2C(N4CCCC4)=O)CN(C(C5=CC=CC=C5)=O)CC(NC(C)(C)C)=O

Room temperature in continental US; may vary elsewhere.

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• [1]. Marcelo Augusto Pereira Januário, et al. Indole Peptidomimetics Show Potent and Selective Activity against Drug-Resistant Plasmodium falciparum. ACS Omega 2026, 11, 20722−20737.