parasite

Niclosamide is a classic salicylanilide antiparasitic drug and a multi-target, low-toxicity, broad-spectrum small-molecule modulator with anthelmintic and antitumor activity. Niclosamide disrupts the parasite’s energy metabolism by uncoupling mitochondrial oxidative phosphorylation, leading to reduced ATP production and ultimately killing the parasite. Niclosamide is a STAT3 inhibitor with an IC₅₀ of 0.25 μM in HeLa cells.

Doxycycline is an orally active tetracycline antibiotic with broad-spectrum inhibitory effects on matrix metalloproteinases (MMPs), possessing both antibacterial and antitumor activities, and is commonly used in inducible gene expression ON-OFF systems.

SQ109 (NSC 722041) is an ethambutol (EMB) derivative and a specific inhibitor of MmpL3, exhibiting potent anti-Mycobacterium tuberculosis activity. SQ109 effectively inhibits the adult stage of the parasite Trypanosoma and kills cells, with an IC₅₀ of 50 ± 8 nM. SQ109 can be used in tuberculosis and antiparasitic research.

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

Palmatine chloride an isoquinoline alkaloid, is an important medicinal herbal extract with diverse pharmacological and biological properties.

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC₅₀= 34.914 ug/mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2, activating caspases as well as cleaving PARP.

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

ABMA is a broad-spectrum inhibitor of intracellular toxins and pathogens, efficiently protecting cells against various pathogens including viruses, intracellular bacteria, and parasites. ABMA selectively acts on host cell late endosomes rather than targeting the toxin or pathogen itself.

Antitrypanosomal agent 2 shows potent and specific antiparasite activities against Trypanosoma brucei.

Cletoquine hydrochloride is a major active metabolite of Hydroxychloroquine. Cletoquine hydrochloride is a Chloroquine derivative and exhibits the ability to against the chikungunya virus (CHIKV). Cletoquine hydrochloride exhibits antimalarial effects.

RR-11a analog (aza-peptide Michael acceptor, 7a) is an inhibitor of asparaginyl endopeptidase with IC₅₀s of 4.5 nM, 4.5 nM and 31 nM for AE1 in Trichomonas Vaginalis, AE in Ixodes ricinus and AE in Schistosoma mansoni, respectively.

Allopurinol riboside is a metabolite of allopurinol with potency against parasites. Allopurinol riboside competitively inhibits the action of purine nucleoside phosphorylase on inosine with a Ki of 277 μM.

Dehydroemetine is an effective antigenic insecticide, which is a synthetic analogue of Emetine dihydrochloride. It can be used to prevent and treat amoeba infections and diseases. It has the effect of treating leishmania infection with skin damage and resistance to metronidazole amoebiosis.

Cipargamin (NITD609) is an effective antimalarial compound. It has an IC₅₀ of appr 1 nM against P. falciparum.

Symetine(L 16726) is a small molecule compound with antiparasitic activity that can be used to study amoebic liver abscesses in guinea pigs.

PPA-904, a specific phenothiazine photosensitizer, is used in photodynamic therapy (PDT).

Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an aromatic diamidine agent effective against various microorganisms, including protozoa (Trypanosoma brucei, Leishmania spp., and Babesia spp.) and fungi (Pneumocystis jirovecii). It is a potent and selective inhibitor of protein tyrosine phosphatases and phosphatase of regenerating liver. Pentamidine dihydrochloride inhibits the parasite Leishmania infantum with an IC₅₀ of 2.5 μM.

DDD85646 is an inhibitor of T. brucei N-myristoyltransferase with a Ki of 1.44 nM, an IC₅₀ of 2 nM and an EC50 of 2 nM. The IC₅₀ of hNMT is 4 nM.

Niridazole (Ambilhar) is an antiparasitic compound belonging to nitroimidazoles. Niridazole is primarily used to treat schistosomiasis, which kills the parasite by interfering with its metabolism. Niridazole rapidly concentrates in the parasite, inhibits egg and sperm production, and inhibits phosphofructokinase activity.

DNDI-6148 has anti-experimental cutaneous leishmaniasis activity and can be used to study visceral leishmaniasis by inhibiting Leishmania protozoa cleavage and polyadenylation-specific factor (CPSF3) endonuclease.

CRK12-IN-2 is a potent inhibitor of CRK12.CRK12-IN-2 inhibits the parasite, with EC50 values of 3.2 and 0.08 nM for Trypanosoma congolense and Trypanosoma vivax, respectively.CRK12-IN-2 can be used for the prevention and treatment of trypanosomiasis in animals.

UCB7362 (GLXC-26743) is an orally available and potent plasmepsin X (PMX) inhibitor with anti-malarial activity.UCB7362 inhibits parasite reproduction.

CpCDPK1/TgCDPK1-IN-3 is a dual inhibitor of CpCDPK1 and TgCDPK1 with an IC₅₀ of 0.003 µM for CpCDPK1 and 0.0036 µM for TgCDPK1. CpCDPK1/TgCDPK1-IN-3 can be used to study infections associated with diseases such as Toxoplasma, Cryptosporidium and Cryptosporidium.

CpCDPK1/TgCDPK1-IN-2 is a dual inhibitor of CpCDPK1 and TgCDPK1 with IC₅₀ values of 12 and 5 nM for CpCDPK1 and TgCDPK1, respectively.CpCDPK1/TgCDPK1-IN-2 can be used in the study of diseases associated with infection of toxoplasmas such as Toxoplasma gondii, Cryptosporidium parvum and C. hominus. CpCDPK1/TgCDPK1-IN-2 can be used to study diseases associated with infections of toxoplasma gondii (T. gondii), Cryptosporidium parvum (C. parvum), and Cryptosporidium hominus (C. hominus).