Plasmodium Inhibitor

DSM265 is a long-duration inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC₅₀ of 8.9 nM. DSM265 can also inhibit the growth of Pf3D7 parasites with an EC₅₀ of 4.3 nM.

Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline chloride elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities. Dehydrocorydaline chloride shows strong anti-malarial effects (IC₅₀ =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.

Cipargamin (NITD609) is an potent antimalarial compound, with an IC₅₀ of appr 1 nM against P. falciparum.

Febrifugine is a quinazolinone alkaloid that inhibits P. falciparum and has antimalarial activity. Febrifugine inhibits bladder cancer by inhibiting DNA synthesis, inducing apoptosis, and reducing steroids.

Cycloguanil (Chlorguanide triazine) hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC₅₀ of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity.

Quinidine sulfate is an antiarrhythmic agent. Quinidine sulfate is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine sulfate is also a K⁺ channel blocker with an IC₅₀ of 19.9 μM. Quinidine sulfate can be used for malaria research.

Piperaquine tetraphosphate tetrahydrate is a bisquinoline antimalarial agent. Piperaquine tetraphosphate tetrahydrate can be used in antimalarial research in combination with Artemisinin.

Sulfadoxine(Sulphadoxine) is a long acting sulfonamide that is used, usually in combination with other agents, for respiratory, urinary tract and malarial infections. Sulfadoxine inhibits HIV replication in peripheral blood mononuclear cells.

Cabamiquine (DDD107498) is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC₅₀ of 1 nM against P. falciparum 3D7. Cabamiquine inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC₅₀ of 2 nM for WT-PfeEF2.

Halofantrine hydrochloride (SKF-102886 hydrochloride; WR-171669 hydrochloride) is a blocker that delays the delayed rectifier potassium current by inhibiting human ERG channels, and it is a potent antimalarial agent with oral activity. Halofantrine hydrochloride inhibits the Cap1-dependent oxidative stress response of Candida albicans, suppresses ROS responses, and enhances the antifungal (Fungal) activity of oxidative damage agents. Halofantrine hydrochloride exhibits antifungal activity in the Galleria mellonella model, and shows antimalarial activity against Plasmodium strains both in vitro and in animal models. Halofantrine hydrochloride can be used in studies related to invasive candidiasis, falciparum malaria, and vivax malaria.

Hydroxychloroquine (sulfate) (Standard) is the analytical standard of Hydroxychloroquine (sulfate). This product is intended for research and analytical applications. Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro.

DL-threo-PDMP hydrochloride is a competitive glucosylceramide synthase (GCS) inhibitor and antimalarial agent. DL-threo-PDMP hydrochloride competitively inhibits the activity of GCS. DL-threo-PDMP hydrochloride restores cisplatin sensitivity in cisplatin-resistant testicular germ cell tumor cells. DL-threo-PDMP hydrochloride blocks the growth of ring-stage Plasmodium falciparum parasites.

AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains (mean IC₅₀=32 nM), Ugandan field isolates (mean ex vivo IC₅₀=64 nM), and murine P. berghei and P. falciparum infections.

Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC₅₀ of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys.

Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak inhibitor of serotonin transporter (SERT) with K_is of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. Antimalarial activities.

Ethylhydrocupreine hydrochloride (Optochin hydrochloride) is a quinine derivate with antimicrobial activity against S. pneumoniae. Ethylhydrocupreine hydrochloride also possesses antimalarial activity against Plasmodium falciparum, with an IC₅₀ of 25.75 nM. Ethylhydrocupreine hydrochloride is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist.

L-Canaline is a nonprotein amino acid stored in many leguminous plants. L-Canaline is a cytotoxic metabolite catalyzed by L-canavanine and its arginase. L-Canaline is a potent and irreversible inhibitor of ornithine aminotransferase. L-Canaline inhibits the growth of the malaria parasite Plasmodium falciparum with an IC₅₀ of 297 nM. L-Canaline has anticancer and antiproliferative effects.

Tuberostemonine is a stenine alkaloid that can be isolated from Stemona tuberosa and Stemona sessifolia. Tuberostemonine is an antimalarial agent that has inhibitory activity against Ferredoxin-NADP⁺ reductases (FNRs) from Plasmodium falciparum (PfFNR). Tuberostemonine can reduce the number of citric acid-induced coughs in guinea pigs. Tuberostemonine decreases bronchoalveolar lavage fluid (BALF), neutrophil and macrophage infiltration and reduces peribronchial and perivascular inflammatory cell infiltration in mouse model of acute lung inflammation. Tuberostemonine has a level of activity as a feeding deterrent .

Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activates p53 signaling, which results in the induction of the apoptosis.

Pafuramidine (DB289) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria.