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DSM502 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM502 exhibits nanomolar potency againsts Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs .
DSM705 hydrochloride, an orally active antimalarial compound, is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 hydrochloride exhibits nanomolar potency against Plasmodium DHODH and Plasmodium parasites (IC50=95, 52 nM for P. falciparum and P. vivax DHODH, respectively), with no inhibition of mammalian DHODHs .
MMV006833 is an inhibitor for Plasmodium falciparum. MMV006833 targets the lipid-transfer protein PfSTART1 and inhibits the development of Plasmodium falciparum at the ring stage .
MMV1557817 is an orally active and potent antimalarial compound. MMV1557817 is a selective, nanomolar inhibitor of both Plasmodium falciparum and Plasmodium vivax aminopeptidases M1 and M17, leading to inhibition of end-stage hemoglobin digestion in asexual parasites .
DSM705 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 exhibits nanomolar potency against Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs. DSM705 is a potent antimalarial compound .
8304-vs is a macrocyclic anti-Plasmodial agent that covalently and irreversibly targets the Plasmodium proteasome. 8304-vs effectively inhibits the growth of Plasmodium falciparum .
NIC is a host invasion inhibitor. NIC can suppress host invasion by interacting with the major invasion-related protein, merozoite surface protein 1 (MSP-1). NIC prevents the invasion of Plasmodium falciparum and Plasmodium vivax into the host .
LysRs-IN-3 (compound 36) is an inhibitor of Plasmodium lysine tRNA synthetase based on ASP3026 (HY-13326), which has a more than seven-fold higher inhibitory effect on the growth of Plasmodium, especially Plasmodium falciparum, than ASP3026 (HY-13326). LysRs-IN-3 can be used in the development of antimalarial drugs .
Antimalarial agent 42 (Compound 2) is an antimalarial agent, that inhibits Plasmodium falciparum in the phase of asexual blood stages (IC50 <0.5μM) and gametocytes (IC50 is 0.14 μM) .
DNMT-IN-3 is an DNA Methyltransferase (DNMT) inhibitor, and plays an antimalarial role with IC50 of 60 nM against Plasmodium falciparum(Plasmodium). DNMT-IN-3 can be used for malaria related research .
DL-threo-PPMP is an inhibitor of sphingosine synthetase in Plasmodium falciparum. DL-threo-PPMP inhibits the activity of sphingosine synthetase by mimicking the substrate sphingosine. This inhibition leads to a rapid decrease in the activity of sensitive sphingosine synthetase, selectively destroying the interconnected tubular network of TVMs in the host cell cytoplasm, and this inhibition also blocks the proliferation of Plasmodium falciparum. DL-threo-PPMP can be used for the study of Plasmodium biology and the search for new antimalarial strategies .
CK-2-68 is an inhibitor for complex III in protozoan mitochondrial respiratory chain, by targeting the alternative NADH dehydrogenase (NDH2) of the malarial parasite Plasmodium. CK-2-68 exhibits antimalaria efficacy, that inhibits Plasmodium falciparum infected erythrocytes with an IC50 of 40 nM .
PfThrRS-IN-1 (compound 11) is a potent inhibitor of Plasmodium falciparum threonyl tRNA synthetase (PfThrRS), with the IC50 value of 0.1 μM. PfThrRS-IN-1 is a potent antimalaria agent .
Anti-infective agent 9 (compound 1) is a Plasmodium falciparum inhibitor (IC50=600 nM), can downregulate pyruvate levels and TCA cycle in Plasmodium. Anti-infective agent 9It has good metabolic stability and low toxicity to human liver cells. The study found, Anti-infective agent 9Potential targets for inhibiting Plasmodium falciparum are not 1-deoxidation-d-xylulose-5-Phosphate synthase (DXPS) .
13,21-Dihydroeurycomanone, a natural compound isolated from Eurycoma longifolia root, possesses anti-parasite activity for Plasmodium falciparum and Toxoplasma gondii .
KDU691, an imidazopyrazine with potent anti-parasitic activity against blood stage schizonts, gametocytes and liver stages, is a Plasmodium PI4K inhibitor. KDU691 selectively inhibits dihydroartemisinin-pretreated Plasmodium falciparum ring-stage parasites .
DHODH-IN-4 (compound 17) is a human and Plasmodium falciparumdihydroorotate dehydrogenase (DHODH) inhibitor, with IC50 values of 4 μM and 0.18 μM for PfDHODH and HsDHODH, respectively. DHODH-IN-4 (compound 17) possess antimalarial activity .
Amythiamicin B is a trisubstituted pyridine thiopeptide with antibiotic properties against Gram-positive bacteria and activity against Plasmodium falciparum .
Ferroquine (Ferrochloroquine), a ferrocenyl analogue of Chloroquine, is an antimalarial agent. Ferroquine shows parasiticidal effect on Plasmodium by inducing oxidative stress and the subsequent destruction of the membrane .
PfDHODH-IN-1 is an analogue of the active metabolite of Leflunomide. PfDHODH-IN-1 is a Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor. PfDHODH-IN-1 has antimalarial activity .
Plm IV inhibitor-2 (compound 3) is a potent digestive vacuole plasmepsins IV (Plm IV) inhibitor with IC50 values of 24 nM, 70 nM and 0.3 μM for Plm IV, II and I, respectively. Plm IV inhibitor-2 can be used to research malaria caused by Plasmodiumparasites .
Antiproliferative agent-56 (Compound 31) is an antimalarial agent, that inhibits Plasmodium falciparum 3D7 (Pf3D7) with an IC50 >12.5 (48h) and 0.03 μM (98h), and reveals a slow-acting property .
S 82-5455 is a floxacrine derivative that exhibits high activity against drug-susceptible strains of Plasmodium berghei induced in mouse and rat blood .
DHFR-IN-5 is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 shows anti-malaria activity .
DHFR-IN-5 hydrochloride is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 hydrochloride shows anti-malaria activity .
Sp-2-Cl-cAMPS is an agonist for PKA with improved membrane permeability and stability to phosphodiesterase. Sp-2-Cl-cAMPS exhibits antimalarial activity, and inhibits the proliferation of Plasmodium falciparum with an EC50 of 4 μM. Sp-2-Cl-cAMPS binds to purified P. falciparum PfPKAr (regulatory subunit of PfPKA) with a Ki of 1.3 µM .
Antimalarial agent 7 is a potent inhibitor of PfATP4. PfATP4 is an essential ion pump on the parasite surface. Antimalarial agent 7 has the potential for the research of human malaria parasite, Plasmodium falciparum .
Pancixanthone A is a xanthone that can be isolated from Garcinia vieillardii. Pancixanthone A has antimalarial activity against chloroquino-resistant strains of Plasmodium falciparum with an IC50 of 1.6 μg/mL .
Isocudraniaxanthone A is a xanthone that can be isolated from Garcinia vieillardii. Isocudraniaxanthone A has antimalarial activity against chloroquino-resistant strains of Plasmodium falciparum with an IC50 of 2.3 μg/mL .
Photosensitizer Pc 4 (NSC-676418) is a photosensitizer, which inhibits Plasmodium falciparum in dark or under red light by disturbing the protein/DNA synthesis, with an IC50 of 24 nM .
OSM-S-106 is a pro-inhibitor and that inhibition of PfAsnRS occurs via enzyme-mediated production of an Asn-OSM-S-106 adduct. OSM-S-106 inhibits protein translation and activates the amino acid starvation response. OSM-S-106 exhibits selective activity against Plasmodium blood and liver stages and low intrinsic clearance by human microsomes .
Bulaquine (CDRI 80/53) is a potent antimalarial agent which is an analogue of Primaquine (HY-12651A). Bulaquine affects multiple metabolism pathways and shows inhibition effect on Plasmodium cynomolgi infection. Bulaquine can be used for the research of malaria .
TDI-8304, a macrocyclic peptide, is a potent, species selective, and noncovalent Plasmodium falciparum (Pf20S) inhibitor. TDI-8304 shows highly selective for Pf20S over human proteasomes .
Genz-669178 is an inhibitor for dihydroorotate dehydrogenase (DHODH) with IC50 of 0.015-0.05 μM in Plasmodium spp.. Genz-669178 inhibits P. berghei, P. falciparum strains 3D7 and Dd2 with IC50 of 0.068, 0.008 and 0.01 μM, respectively. Genz-669178 exhibits anti-malarial efficacy in P. berghei-infected mice with ED50 of 13-21 mg/kg/day. Genz-669178 exhibits good pharmacokinetic characteristics in mice .
GLUT1-IN-2 (compound 17) is a GLUT1 inhibitor with an IC50 value of 12 μM. GLUT1-IN-2 shows inhibitory effect to Plasmodium falciparum hexose transporter PfHT with an IC50 value of 13 μM. GLUT1-IN-2 can be used for the research of infection .
Digitolutein is a natural product that can be isolated from the stem bark and the roots of Morinda lucida Benth. Digitolutein effectively inhibits the growth of Plasmodium falciparum with an IC50 value of 12.92 μg/mL. Digitolutein can be used for the research of infection .
DHODH-IN-8 (Compound 27) is an inhibitor of human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) with IC50s of 0.13 μM and 47.4 μM, and Kis of 0.016 μM and 5.6 μM, respectively. DHODH-IN-8 has antimalarial activity .
PfDHODH-IN-2, a dihydrothiophenone derivative (Compound 11), is a potent Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor with an IC50 of 1.11 µM. PfDHODH-IN-2 acts as an antimalarial agent and can be used for the research of malaria .
Cheilanthifoline, an alkaloid, is isolated from Corydalis calliantha. Cheilanthifoline exhibits antiplasmodial activities against Plasmodium falciparum, with IC50s of 0.90 μg/mL and 1.22 μg/mL for wild type (TM4) and multidrug resistant (K1) strains, respectively .
Halofantrine (SKF-102886 free base) is a highly lipophilic antimalarial active against Chloroquine-resistant strains of Plasmodium falciparum . Halofantrine blocks HERG potassium channels .
Nitidanin ((±)-Nitidanin) is an antimalarial and antiviral compound that can be isolated from the wood of Xanthoxylum nitidun D. C. Nitidanin is shows IC50 values of 21.2 and 18.4 μM for D6 and W2 clones of Plasmodium falciparum, respectively. Nitidanin can be used for the research of malaria and virus infection .
Tebuquine (WR228258), a 4-aminoquinoline, is a potent antimalarial agent. Tebuquine is active against the Chloroquine (HY-17589A) sensitive HB3 strain and the Chloroquine resistant K1 strain of Plasmodium falciparum with IC50s of 0.9 nM and 20.8 nM, respectively .
Aminoacyl tRNA synthetase-IN-3 (compound 36K3) is an inhibitor of lysine tRNA synthetase (PfLysRS) from Plasmodium falciparum (IC50=59.2 nM), which inhibits the activity of PfLysRS by occupying the ATP binding site and L-lysine binding site of PfLysRS. Aminoacyl tRNA synthetase-IN-3 can be used in the development of antimalarial drugs .
Antimalarial agent 41 (Compound 17) exhibits antimalarial activity, which inhibits Plasmodium falciparum with an IC50 of 40 nM (NF54 strain) and 76 nM (K1 strain). Antimalarial agent 41 is an inhibitor for P. falciparum phosphatidylinositol-4-kinase β (Pf PI4K) and hERG channel, with an IC50 of 53 nM and 3 μM. Antimalarial agent 41 exhibits cytotoxicity to CHO cells with an IC50 of 34 μM. Antimalarial agent 41 ameliorates the malaria infection and exhibits good pharmacokinetic characters in mouse models .
DL-threo-PPMP hydrochloride is an inhibitor of sphingosine synthetase in Plasmodium falciparum. DL-threo-PPMP hydrochloride inhibits the activity of sphingosine synthetase (sphingosine synthetase) by binding to a substrate that mimics sphingosine. This inhibition leads to a rapid decline in sensitive sphingomyelin synthase (SSS) activity, selectively disrupting the interconnected tubular network of TVM in the cytoplasm of the host cell, and this inhibition also blocks the proliferation of the parasite. DL-threo-PPMP hydrochloride can be used in the study of malaria parasite biology and the search for new antimalarial strategies .
Pheanthine (Compound 2) is an antiplasmodial agent, that inhibits chloroquine-resistant Plasmodium falciparum K-1 (IC50 is 0.8 μM) and chloroquine-sensitive P. falciparum strain NF54 A19A (IC50 of 0.03 μM). Pheanthine exhibits low cytotoxicity in human lung fibrosblast (MRC-5, IC50 is 11.2 μM) and macrophages (PMM, IC50 is 8 μM) .
Nanaomycin A is the first selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells . Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM .
SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G .
SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 quarterhydrate shows no inhibitory activity against cathepsin G .
JMI-346 is a potent PfFP-2(Plasmodium falciparum falcipain-2 protease) inhibitor. JMI-346 inhibits the growth of CQ S (3D7; IC50=13 µM) and CQ R (RKL-9; IC50=33 µM) strains of P. falciparum. JMI-346 has the potential to be used as an anti-malarial agent .
PAM 1392 is active orally against Plasmodium berghei in mice, P. cynofologi and P. knowlesi in monkeys and Trypanosoma cruzi in tissue cultures of mice, and hemolytic streptococci in vitro. PAM 1392 has antimalarial and antitrypanosomal activities, which is proming for rasearch of drug-resistant malaria .
2-Butenoyl coenzyme A (lithium), an active compound, can be used as a substrate for plasmodium falciparum enyl-ACP reductases and other enyl-CoA reductases. 2-Butenoyl coenzyme A lithium can be used as a substrate analogue to study the kinetics of β-hydroxyacyl-acyl-carrier protein (ACP) dehydratase (FabZ) .
Quinoprazine is a potent inhibitor of Vaccinia virus DNA synthesis with an IC50 value of 10 μM. Quinoprazine has antimalarial activity against Plasmodium berghei and also displays antiprion potency, significantly decreases PrP S c levels - .
Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage .
D44 is a PlasmodiumFKBP35 inhibitor that selectively inhibits the FKBD35PPIase activity, with PPIaseIC50 values of 132 nM and 125 nM for Plasmodium falciparum and Plasmodium vivax, respectively. D44 exhibits antiplasmodium activity and can be used in research related to infectious diseases .
Phebestin is a compound with antimalarial activity that has an inhibitory effect on Plasmodium and has shown good results in in vitro and in vivo experiments. It can also bind to related enzymes of Plasmodium.
Antimalarial agent 33 (compound 5g) has antiplasmodial activity against erythrocytic and hepatic stages of Plasmodium with an EC50 of 1.1 μM for K1 P. falciparum strain. Antimalarial agent 33 demonstrats enhanced microsomal stability (T1/2=29 min). Antimalarial agent 33 has no significant cytotoxicity against primary hepatocytes .
Phomoxanthone A is a xanthone dimer, which can be isolated from Phomopsis. Phomoxanthone A exhibits antimalarial and antitubercular activities against Plasmodium falciparum (K1, multidrug-resistant strain, IC50 is 0.11 µg/mL) and Mycobacterium tuberculosis (H37Ra strain, MIC is 0.50 µg/mL). Phomoxanthone A exhibits cytotoxicity in cells KB, BC-1 and Vero, IC50 is 0.99, 0.51 and 1.4 µg/mL, respectively .
Euquinine is an odorless salt that can be used as
a substitute for quinine. Euquinine has anti-Plasmodium falciparum activity.
Euquinine can be used for the study of multidrug resistance and bioavailability
of Plasmodium falciparum .
JMI-105 is a potent PfFP-2(Plasmodium falciparum falcipain-2 protease) inhibitor. JMI-105 inhibits the growth of CQ S (3D7; IC50=8.8 µM) and CQ R (RKL-9; IC50=14.3 µM) strains of P. falciparum. JMI-105 significantly decreases parasitemia and prolonged host survival in a murine model with P. berghei ANKA infection. JMI-105 has the potential to be used as an anti-malarial agent .
Mirincamycin (hydrochloride) (U-24729 A), a compound used to inhibit malaria, has a protective effect against the early liver stages of Plasmodium but fails to kill dormant liver stages of Plasmodium in a rhesus monkey model.
Purine phosphoribosyltransferase-IN-2 is a potent inhibitor of the Plasmodium falciparum ((Pf)), Plasmodium vivax ((Pv)) and Trypanosoma brucei ((Tbr)) 6-oxopurine phosphoribosyltransferase (PRT), with Kis of 30, 20 and 2 nM, respectively .
Nopol is a quinoline derivative based on nopol that has inhibitory activity against the asexual blood stage of Plasmodium falciparum. Derivatives with different structures have different activities against different Plasmodium strains, and some derivatives have submicromolar EC50 values in specific strains.
Primaquine-d3 (diphosphate) is the deuterium labeled Primaquine diphosphate. Primaquine Diphosphate (Primaquine phosphate), an 8-aminoquinoline, exerts a broad spectrum of activities against various stages of parasitic malaria. Primaquine Diphosphate remains as the only agent that destroys late hepatic stages and latent tissue forms of Plasmodium vivax and Plasmodium ovale[1][2].
Epoxyazadiradione is a limonoid purified from neem (Azadirachta indica) fruits. Epoxyazadiradione inhibits the tautomerase activity of MIF of both human (huMIF) and malaria parasites (Plasmodium falciparum (PfMIF) and Plasmodium yoelii (PyMIF)) non-competitively in a reversible fashion (Ki, 2.11-5.23 μM). Epoxyazadiradione has the potential against proinflammatory reactions induced by MIF of both malaria parasites and human .
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 .
trans-Cinnamic anhydride is a Parasite inhibitor tnat can be isolated from Cinnamomum zeylanicum and exhibits moderate activity against Plasmodium falciparum .
Floxacrine (HOE-991) is a dihydroacridinedione derivative with antimalarial activity. Floxacrine can be used to study its activity against different Plasmodium species .
RO-09-4609 exhibits antimicrobial activity, that inhibits Candida albicans, Trypanosoma brucei and Plasmodium vivax through inhibition of N-myristoyl transferase .
MMV390048 is a representative of a new chemical class of PlasmodiumPI4K inhibitor (Kdapp=0.3 µM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns. MMV390048 is an antimalarial agent .
Brevicompanine B, a diketopiperazine alkaloid, is an antiplasmodial agent. Brevicompanine B is active against the malaria parasite Plasmodium falciparum 3D7 IC50 of 35 mg/mL .
trans-Clopenthixol ((E)-Clopenthixol) dihydrochloride is an antibiotic agent, without neuroleptic effect. trans-Clopenthixol can be used to inhibit Pseudomonas aeruginosa and Plasmodium falciparum in vitro .
TCMDC-137332 is a compound that exhibits antimalarial activity against Plasmodium falciparum with an IC50 value of 7 nM. TCMDC-137332 can be utilized for the research of malaria .
SpdSyn binder-1 is a weak binder, which binds in the active site of plasmodium falciparum spermidine synthase. SpdSyn binder-1 can be used for the research of malaria .
Azlocillin sodium salt (Sodium azlocillin), a semisynthetic penicillin, is a broad spectrum β-lactam antibiotic. Azlocillin sodium salt shows antipseudomonal activity, and also potent against the malarial parasitePlasmodium falciparum .
Artelinic acid, a derivative of Artemisinin, is an antimalarial agent for the treatment of multidrug resistant strains of Plasmodium falciparum. Artelinic acid can be administered by various routes of administration, including intravenous, intramuscular and oral routes .
1-(26-Hydroxyhexacosanoyl)-glycerol is a potent antimalarial agent. 1-(26-Hydroxyhexacosanoyl)-glycerol shows antimalarial activity with an IC50 value of 9.48 µM for Plasmodium falciparum .
PfPKG-IN-2 (compound 53) is a potent Plasmodium falciparum cGMP-dependent protein kinase (PfPKG) inhibitor with an IC50 value of 13 nM. PfPKG-IN-2 shows antiparasitic activity .
Arterolane (OZ 277) (maleate) is an orally active antimalarial. Arterolane exhibits potent activity against erythrocytic stages of P. falciparum and Plasmodium vivax. Arterolane (maleate) is promising for research of falciparum malaria .
ELQ-596 is a quinolone derivative, that exhibits antimicrobial activity against several protozoan parasites, including the intraerythrocytic parasites Plasmodium and Babesia. ELQ-596 attenuates babesiosis in immunosuppressed mice .
ELQ-650 is a quinolone derivative, that exhibits antimicrobial activity against several protozoan parasites, including the intraerythrocytic parasites Plasmodium and Babesia. ELQ-650 attenuates babesiosis in immunosuppressed mice .
Decoquinate is a quinolone derivative that can be used for research of coccidiosis in domestic ruminants. Decoquinate also has potent activity against both Plasmodium hepatic development and red cell replication .
Z-Antiepilepsirine is an amide alkaloid that can be found in Piper capense L.f. Z-Antiepilepsirine shows antiplasmodial activity with an IC50 value of 27 µM for W2 strain of Plasmodium falciparum .
MMV666693 is a translation inhibitor specific for Plasmodium falciparum. MMV666693 has low cytotoxicity in human fibroblasts (IC50>32 µM) and can be used in the development of antimalarial drugs .
PfDHODH-IN-3 (compound 2) is an orally active PfDHODH inhibitor with strong antimalarial activity (IC50=47 nM). PfDHODH-IN-3 can inhibit the growth of Plasmodium in animals .
CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K(Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy .
CWHM-1008 is a potent and orally active antimalarial agent, with EC50 values of 46 and 21 nM against agent-sensitive Plasmodium falciparum 3D7 and drug-resistant Dd2 strains, respectively .
Chaparrinone is a quassinoid that can be isolated from the root of Eurycoma harmandiana. Chaparrinone has antimalarial and cytotoxic activities against Plasmodium falciparum and P-388 cells (IC50: 0.037 and 0.34 μg/mL respectively) .
Phosphodiesterase-IN-1 (Compound 7) is a phosphodiesterase (PDE) inhibitor with anti-Plasmodium activity. Phosphodiesterase-IN-1 has antiproliferative activity against P. falciparum (strain 3D7) with an IC50 value of 0.64 μM .
PfFAS-II inhibitor 1 (Compound 3) is a Plasmodium falciparum type II fatty acid biosynthesis pathway (PfFAS-II) inhibitor, with an IC50 of 0.63 μM for PfFabI enzyme. PfFAS-II inhibitor 1 has antimalarial activity .
DSM74 (compound 21) is an orally active and potent antimalarial inhibitor of PfDHODH (IC50=0.28 μM) and PbDHODH (IC50=0.38 μM). DSM74 inhibits the growth of Plasmodium in animals .
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 .
LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC50s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) and Cryptosporidium parvum lysyl-tRNA synthetase (CpKRS), respectively .
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 .
Zymolyase, Arthrobacter luteus, is a zymolyase mainly found in Arthrobacter luteus. Enzyme, an enzyme with beta-1,3 glucanase activity, removes the electron-dense outer layer of the Plasmodium karinii cell wall, exposing an electron-lucent layer .
Purine phosphoribosyltransferase-IN-1 (Compound (S,R)-48) is a potent inhibitor of the Plasmodium falciparum (Pf), P. vivax (Pv) and Trypanosoma brucei (Tbr) 6-oxopurine purine phosphoribosyltransferases (PRTs), with Ki values of 50, 20, and 2 nM, respectively .
FNDR-20123 free base 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 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations .
Hexyl gallates (Hexyl 3,4,5-trihydroxybenzoate) shows antibacterial activity and inhibits the production of rhamnolipid and pyocyanin by inhibiting RhlR . Hexyl gallate, a alkyl ester derivative of gallic acid, exhibits potent antimalarial activity against Plasmodium falciparum, with IC50 of 0.11 mM .
Azlocillin (sodium salt) (Standard) is the analytical standard of Azlocillin (sodium salt). This product is intended for research and analytical applications. Azlocillin sodium salt (Sodium azlocillin), a semisynthetic penicillin, is a broad spectrum β-lactam antibiotic. Azlocillin sodium salt shows antipseudomonal activity, and also potent against the malarial parasitePlasmodium falciparum .
Ganaplacide (KAF156) is a first-in-class,
orally active imidazolopiperazine antimalarial agent.
Ganaplacide is active against a broad range of Plasmodium
species, including drug-resistant parasites. Ganaplacide is parasiticidal
against both asexual and sexual blood stages as well as the liver stages of the
parasite .
Ganaplacide (KAF156) hydrochloride is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide hydrochloride is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide hydrochloride is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite .
Gallinamide A TFA is a linearly depositing peptide and a potent inhibitor of cathepsin L (CatL) (IC50: 17.6 pM). Gallinamide A TFA inhibits SARS-CoV-2 infection by inhibiting CatL (EC50: 28 nM). Gallinamide A TFA also inhibits Plasmodium falciparum (IC50: 50 nM) .
Decoquinate (Standard) is the analytical standard of Decoquinate. This product is intended for research and analytical applications. Decoquinate is a quinolone derivative that can be used for research of coccidiosis in domestic ruminants. Decoquinate also has potent activity against both Plasmodium hepatic development and red cell replication .
KAR425 is a potent and orally active antimalarial agent. KAR425 shows antimalarial activity against the Chloroquine-sensitive (CQS) D6, the Chloroquine-resistant (CQR) Dd2, and 7G8 strains of Plasmodium falciparum, with IC50 values of 62 nM, 55 nM, and 60 nM, respectively .
PI4KIIIbeta-IN-11 is an inhibitor of PI4KIIIβ, with a mean pIC50 value of at least 9.1. PI4KIIIβ plays a key role in diseases research of RNA viruses and Plasmodium falciparum .
Phytol ((E)-Phytol) is an orally active diterpenoid alcohol that can be extracted from chlorophyll. Phytol has antioxidant, anti-inflammatory, anti-schistosomiasis and antibacterial activities .
Sporogen AO-1 is a fungal metabolite originally isolated from the fungusAspergillus oryzae. Sporogen AO-1 has significant antimalarial activity againstplasmodium falciparum, with an IC50 value of 1.53 μM, and also has certain cytotoxicity .
Guanfu base H (Atisinium chloride) is a diterpenoid alkaloid isolated from Aconitum coreanum and has antiplasmodial activity against the malarial Plasmodium falciparum strains TM4/8.2 (wild type) and K1CB1 with IC50 values of 4 μM and 3.6 μM, respectively .
Miaosporone A, an angucyclic quinone, exhibits antimalarial activity against Plasmodium falciparum K1 and antibacterial activity against Mycobacterium tuberculosis with respective IC50 values of 2.5 and 2.4 μM and displays cytotoxic activities against both cancerous (MCF-7 and NCI-H187) and nonmalignant (Vero) cells .
SNX-0723 is a potent Hsp90 Inhibitor with anti-Plasmodium activity. SNX-0723 shows high binding affinity for HsHsp90 and PfHsp90 with Kis of 4.4 and 47 nM, respectively. SNX-0723 inhibits liver-stage P. berghei ANKA parasites with the EC50 of 3.3 μM .
MMV688533 is an antimalarial agent with rapid anti-plasmodial activity and effective single-dose activity against Plasmodium falciparum infection in humanized mouse models. MMV688533 can inhibit the activity of asexual blood stage parasites with an IC50 value of 1.3 nM. MMV688533 exhibits excellent pharmacokinetic properties and safety .
8-Deoxygartanin, a prenylated xanthones from G. mangostana, is a selective inhibitor of butyrylcholinesterase (BChE) . 8-Deoxygartanin exhibits antiplasmodial activity with an IC50 of 11.8 μM for the W2 strain of Plasmodium falciparum . 8-Deoxygartanin inhibits NF-κB (p65) activation with an IC50 of 11.3 μM .
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 .
Ethylhydrocupreine (Optochin) is a quinine derivate with antimicrobial activity against S. pneumoniae. Ethylhydrocupreine also possesses antimalarial activity against Plasmodium falciparum, with an IC50 of 25.75 nM. Ethylhydrocupreine is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist .
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 .
Atovaquone (Standard) is the analytical standard of Atovaquone. This product is intended for research and analytical applications. Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome bc1 complex. Atovaquone is against human and P. falciparum cytochrome bc1 activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia .
Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome bc1 complex. Atovaquone is against human and P. falciparum cytochrome bc1 activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia .
PfGSK3/PfPK6-IN-2 is a potent dual PfGSK3/PfPK6(Plasmodium falciparum GSK3/PK6) inhibitor (IC50: 172 nM and 11 nM respectively). PfGSK3/PfPK6-IN-2 can be used in the research of Malaria .
MMV009085 is a potent PfHT1 (Plasmodium falciparum hexose transporter)-specific inhibitor and a potential anti-malarial agent . MMV009085 is also a human glucose transporter inhibitor, it has high potency in inhibiting both glucose uptake (IC50: 2.6 μM in glucose uptake assay) and growth of the parasites (EC50: 1.23±0.04 μM against 3D7) .
Sulfadoxine-d3 is a deuterium labeled Sulfadoxine (HY-B0439). Sulfadoxine is a sulfonamide that is used, usually in combination with Pyrimethamine (HY-18062), for multidrug-resistant Plasmodium falciparum and P. vivax inhibition. Unlike PYR, Sulfadoxine has no impact on HIV replication or MT-2 cell cycle progression. But also Sulfadoxine exhibits suppression on respiratory, and urinary tract infections[1][2][3][4].
PfSUB1-IN-1 (compound 4c) is a plasmodium falciparum subtilisin-like serine protease 1 (PfSUB1) Inhibitor (IC50: 15 nM). PfSUB1 is an antimalarial target. PfSUB1-IN-1 inhibits the growth of a genetically modified P. falciparum line expressing reduced levels of PfSUB1 13-fold more efficiently compared to a wild-type parasite line .
Ethylhydrocupreine (hydrochloride) (Standard) is the analytical standard of Ethylhydrocupreine (hydrochloride). This product is intended for research and analytical applications. 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 .
Antimalarial agent 25 is an orally active 1,4-naphthoquinones derivative with antimalarial activity. Antimalarial agent 25 shows cytotoxicity against P. falciparum. Antimalarial agent 25 inhibits P. burghei induced parasitemia in vivo .
Antiparasitic agent-17 (compound 5u) is an orally active antiparasitic agent. Antiparasitic agent-17 inhibits Chloroquine sensitive (Pf3D7) and Chloroquine resistant (PfK1) strain with IC50s of 0.96 μM and 1.67 μM, respectively .
ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial .
DHFR-IN-20 (Compound LA1) is a Plasmodium falciparum dihydrofolate reductase (DHFR) inhibitor, with Kis of 0.16, 0.30, 6.6 nM for PfDHFR-WT, PfDHFR-QM, HsDHFR. DHFR-IN-20 has antimalarial activities (IC50: 1.4 nM and 1.6 μM for P. falciparum carrying the wild-type (TM4/8.2) and the quadruple mutant (V1/S) PfDHFR enzyme .
beta-Mangostin (β-Mangostin) is a xanthone compound present in Cratoxylum arborescens, with antibacterial and antimalarial activities. beta-Mangostin exhibits antimycobacterial activity against Mycobacterium tuberculosis with an MIC of 6.25 μg/mL. beta-Mangostin possesses in vitro antimalarial activity against Plasmodium falciparum, with an IC50 of 3.00 μg/mL. beta-Mangostin has potent anticancer activity against various cancers (such as hepatocellular carcinoma, leukaemic) .
Antileishmanial agent-21 (compound 4e) is an antileishmanial agent that targets the Leishmania pteridine reductase 1 (Lm-PTR1). Antileishmanial agent-21 has an anti-folate mechanism, and folic acid and leucovorin can reverse the anti-leishmanial activity of Antileishmanial agent-21. Antileishmanial agent-21 inhibits the Chloroquine (HY-17589A)-resistant strain of Plasmodium falciparum (RKL9) with an IC50 of 0.0198-0.096 μM .
SJ000025081 is a dihydropyridine and acts as a potent antimalarial agent. SJ000025081 results in an obvious suppression of the parasitemia in a murine malaria model infected with P. yoelii .
Methylenetanshinquinone is a natural compound with antiplasmodial, antitrypanosomal and antioxidative activities. Methylenetanshinquinone can be used for the research of parasite infection .
MMV019313 is a potent, non-bisphosphonate inhibitor of farnesyl/geranylgeranyl diphosphate synthase (FPPS/GGPPS) with an IC50 of 0.82 µM. MMV019313 has activity against P. falciparum (Parasite) .
Deacylketoconazole (N-Deacetylketoconazole; R-39519) is an orally active metabolite of Ketoconazole (HY-B0105). Deacylketoconazole exhibits antifungal and antibacterial activity. Deacylketoconazole is cytotoxic in rats hepatocyte .
Micrococcin P1 is a macrocyclic peptide antibiotic and is a potent hepatitis C virus (HCV) inhibitor with an EC50 range of 0.1-0.5 μM . Micrococcin P1 has in vitro antibacterial activity against Gram-positive bacterial strains. The MIC values of Micrococcin P1 against S. aureus 1974149, E. faecalis 1674621 and S. pyogenes 1744264 are 2 μg/mL, 1 μg/mL and 1 μg/mL, respectively . Micrococcin P1 is also a potent inhibitor of the malaria parasitePlasmodium falciparum .
TCMDC-135051 is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 has antiparasiticidal activity (EC50=320 nM) .
TCMDC-135051 hydrochloride is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 hydrochloride prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 hydrochloride has antiparasiticidal activity (EC50=320 nM) .
TCMDC-135051 TFA is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 TFA prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 TFA has antiparasiticidal activity (EC50=320 nM) .
Lactucin is an anti-inflammatory agent. Lactucin induces cancer cell apoptosis. Lactucin also shows analgesic, anticancer and antimalarial activities .
Lactucin (Standard) is the analytical standard of Lactucin. This product is intended for research and analytical applications. Lactucin is an anti-inflammatory agent. Lactucin induces cancer cell apoptosis. Lactucin also shows analgesic, anticancer and antimalarial activities [4].
Borrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor which is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei . Borrelidin is an inhibitor of Cdc28/Cln2 of the budding yeast, with an IC50 of 24 μM . Borrelidin is a potent angiogenesis inhibitor, with an IC50 of 0.8 nM. Borrelidin induces apoptosis in the tube-forming cells . Borrelidin has strong antimalarial activities, with IC50s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum, respectively .
CR-1-31-B is a synthetic rocaglate and a potent eIF4A inhibitor. CR-1-31-B exhibits powerful inhibitory effects over eIF4A by perturbing the interaction between eIF4A and RNA, sequentially impeding initiation during protein synthesis. CR-1-31-B perturbs association of Plasmodium falciparum eIF4A (PfeIF4A) with RNA. CR-1-31-B induces apoptosis of neuroblastoma and gallbladder cancer cells .
HDAC-IN-76 (compound 6i) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-76 IC50 values of 30 nM and 98 nM for Pf3D7 (chloroquine (HY-17589A) drug-susceptible strain) and PfDd2 (chloroquine (HY-17589A) drug-resistant strain), has a highly potent antimalarial activity against asexual blood-stage Plasmodium, respectively, and exhibits selective inhibition against parasites, with IC50 values of 7 nM and 9 nM for human HDAC1 and HDAC6, respectively, while inhibiting PfHDAC1 .
Anti-inflammatory agent 40 is a potential and orally active anti-malarial and anti-inflammatory agent. Anti-inflammatory agent 40 inhibits carrageenan induced paw swelling in vivo.
Antiparasitic agent-22 (Compound 24) is a pan antiparasitic agent, that inhibits T. Brucei, L. infantum, L. tropica promastigotes (IC50 of 2.41, 5.95, 8.98 μM), L. infantum amastigotes (IC50 of 8.18 μM) and P. falciparum W2 strain (IC50 of 0.155 μM). Antiparasitic agent-22 exhibits low cytotoxicity against THP1, with CC50 of 64.16 μM .
FR900098 sodium is an antimalarial agent that inhibits 1-deoxy-d-xylulose-5-phosphate (DXP) reductoisomerase. FR900098 sodium has no significant acute toxicity or genotoxicity, and does not have the ability to cause chromosome breakage or heterogeneity. FR900098 sodium has no effect on bone marrow red blood cells in NMRI mice .
FR900098 is an antimalarial agent that inhibits 1-deoxy-d-xylulose-5-phosphate (DXP) reductoisomerase. FR900098 has no significant acute toxicity or genotoxicity, and does not have the ability to cause chromosome breakage or heterogeneity. FR900098 has no effect on bone marrow red blood cells in NMRI mice .
A parasite is an organism that lives on or in a host organism and gets its food from or at the expense of its host. Parasites of humans include protozoans, helminths, and ecto-parasites (organisms that live on the external surface of a host). They are responsible for many diseases and are transmitted to their hosts most often through the ingestion of contaminated food, water or through the bite of an arthropod (e.g., a fly or tick), which can act as an intermediate host and as a vector. Parasitic diseases of humans are a major global health problem causing significant morbidity and mortality, especially in developing countries. Each year there are hundreds of millions of people infected with disease-causing parasites, particularly in tropical and subtropical regions of the world, resulting in an estimated one million deaths. Therefore, there is a dire need of novel anti-parasitic drugs.
MCE has a unique collection of 482 compounds with validated anti-parasitic activity which offer researchers an opportunity to screen novel anti-parasitic targets.
2-Butenoyl coenzyme A (lithium), an active compound, can be used as a substrate for plasmodium falciparum enyl-ACP reductases and other enyl-CoA reductases. 2-Butenoyl coenzyme A lithium can be used as a substrate analogue to study the kinetics of β-hydroxyacyl-acyl-carrier protein (ACP) dehydratase (FabZ) .
Dabcyl-LNKRLLHETQ-Edans (Fluorigenic PEXEL peptide) is a biological active peptide. (This FRET substrate peptide for Plasmepsin V (PMV) is derived from the conserved Plasmodium Export Element (PEXEL) motif of Histidine-Rich Protein II (HRPII). PMV is an ER aspartic protease that recognizes and cleaves the RXL sequence within the PEXEL motif of proteins exported by human malaria parasite Plasmodium falciparum, allowing them to translocate into host erythrocytes.)
Ac-{Cpg}-Thr-Ala-{Ala(CO)}-Asp-{Cpg}-NH2 (compound 40) is a potent Plasmodium subtilisin-like protease 1 (SUB1) inhibitor. SUB1-IN-1 shows IC50 values of 12 nM and 10 nM against P. vivax and P. falciparum SUB1 (Pv- and PfSUB1), respectively .
13,21-Dihydroeurycomanone, a natural compound isolated from Eurycoma longifolia root, possesses anti-parasite activity for Plasmodium falciparum and Toxoplasma gondii .
Digitolutein is a natural product that can be isolated from the stem bark and the roots of Morinda lucida Benth. Digitolutein effectively inhibits the growth of Plasmodium falciparum with an IC50 value of 12.92 μg/mL. Digitolutein can be used for the research of infection .
Amythiamicin B is a trisubstituted pyridine thiopeptide with antibiotic properties against Gram-positive bacteria and activity against Plasmodium falciparum .
Pancixanthone A is a xanthone that can be isolated from Garcinia vieillardii. Pancixanthone A has antimalarial activity against chloroquino-resistant strains of Plasmodium falciparum with an IC50 of 1.6 μg/mL .
Isocudraniaxanthone A is a xanthone that can be isolated from Garcinia vieillardii. Isocudraniaxanthone A has antimalarial activity against chloroquino-resistant strains of Plasmodium falciparum with an IC50 of 2.3 μg/mL .
Cheilanthifoline, an alkaloid, is isolated from Corydalis calliantha. Cheilanthifoline exhibits antiplasmodial activities against Plasmodium falciparum, with IC50s of 0.90 μg/mL and 1.22 μg/mL for wild type (TM4) and multidrug resistant (K1) strains, respectively .
Nitidanin ((±)-Nitidanin) is an antimalarial and antiviral compound that can be isolated from the wood of Xanthoxylum nitidun D. C. Nitidanin is shows IC50 values of 21.2 and 18.4 μM for D6 and W2 clones of Plasmodium falciparum, respectively. Nitidanin can be used for the research of malaria and virus infection .
Pheanthine (Compound 2) is an antiplasmodial agent, that inhibits chloroquine-resistant Plasmodium falciparum K-1 (IC50 is 0.8 μM) and chloroquine-sensitive P. falciparum strain NF54 A19A (IC50 of 0.03 μM). Pheanthine exhibits low cytotoxicity in human lung fibrosblast (MRC-5, IC50 is 11.2 μM) and macrophages (PMM, IC50 is 8 μM) .
2-Butenoyl coenzyme A (lithium), an active compound, can be used as a substrate for plasmodium falciparum enyl-ACP reductases and other enyl-CoA reductases. 2-Butenoyl coenzyme A lithium can be used as a substrate analogue to study the kinetics of β-hydroxyacyl-acyl-carrier protein (ACP) dehydratase (FabZ) .
Phomoxanthone A is a xanthone dimer, which can be isolated from Phomopsis. Phomoxanthone A exhibits antimalarial and antitubercular activities against Plasmodium falciparum (K1, multidrug-resistant strain, IC50 is 0.11 µg/mL) and Mycobacterium tuberculosis (H37Ra strain, MIC is 0.50 µg/mL). Phomoxanthone A exhibits cytotoxicity in cells KB, BC-1 and Vero, IC50 is 0.99, 0.51 and 1.4 µg/mL, respectively .
Epoxyazadiradione is a limonoid purified from neem (Azadirachta indica) fruits. Epoxyazadiradione inhibits the tautomerase activity of MIF of both human (huMIF) and malaria parasites (Plasmodium falciparum (PfMIF) and Plasmodium yoelii (PyMIF)) non-competitively in a reversible fashion (Ki, 2.11-5.23 μM). Epoxyazadiradione has the potential against proinflammatory reactions induced by MIF of both malaria parasites and human .
trans-Cinnamic anhydride is a Parasite inhibitor tnat can be isolated from Cinnamomum zeylanicum and exhibits moderate activity against Plasmodium falciparum .
Brevicompanine B, a diketopiperazine alkaloid, is an antiplasmodial agent. Brevicompanine B is active against the malaria parasite Plasmodium falciparum 3D7 IC50 of 35 mg/mL .
1-(26-Hydroxyhexacosanoyl)-glycerol is a potent antimalarial agent. 1-(26-Hydroxyhexacosanoyl)-glycerol shows antimalarial activity with an IC50 value of 9.48 µM for Plasmodium falciparum .
Z-Antiepilepsirine is an amide alkaloid that can be found in Piper capense L.f. Z-Antiepilepsirine shows antiplasmodial activity with an IC50 value of 27 µM for W2 strain of Plasmodium falciparum .
Chaparrinone is a quassinoid that can be isolated from the root of Eurycoma harmandiana. Chaparrinone has antimalarial and cytotoxic activities against Plasmodium falciparum and P-388 cells (IC50: 0.037 and 0.34 μg/mL respectively) .
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 .
Gallinamide A TFA is a linearly depositing peptide and a potent inhibitor of cathepsin L (CatL) (IC50: 17.6 pM). Gallinamide A TFA inhibits SARS-CoV-2 infection by inhibiting CatL (EC50: 28 nM). Gallinamide A TFA also inhibits Plasmodium falciparum (IC50: 50 nM) .
Phytol ((E)-Phytol) is an orally active diterpenoid alcohol that can be extracted from chlorophyll. Phytol has antioxidant, anti-inflammatory, anti-schistosomiasis and antibacterial activities .
Sporogen AO-1 is a fungal metabolite originally isolated from the fungusAspergillus oryzae. Sporogen AO-1 has significant antimalarial activity againstplasmodium falciparum, with an IC50 value of 1.53 μM, and also has certain cytotoxicity .
Guanfu base H (Atisinium chloride) is a diterpenoid alkaloid isolated from Aconitum coreanum and has antiplasmodial activity against the malarial Plasmodium falciparum strains TM4/8.2 (wild type) and K1CB1 with IC50 values of 4 μM and 3.6 μM, respectively .
Miaosporone A, an angucyclic quinone, exhibits antimalarial activity against Plasmodium falciparum K1 and antibacterial activity against Mycobacterium tuberculosis with respective IC50 values of 2.5 and 2.4 μM and displays cytotoxic activities against both cancerous (MCF-7 and NCI-H187) and nonmalignant (Vero) cells .
8-Deoxygartanin, a prenylated xanthones from G. mangostana, is a selective inhibitor of butyrylcholinesterase (BChE) . 8-Deoxygartanin exhibits antiplasmodial activity with an IC50 of 11.8 μM for the W2 strain of Plasmodium falciparum . 8-Deoxygartanin inhibits NF-κB (p65) activation with an IC50 of 11.3 μM .
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 .
beta-Mangostin (β-Mangostin) is a xanthone compound present in Cratoxylum arborescens, with antibacterial and antimalarial activities. beta-Mangostin exhibits antimycobacterial activity against Mycobacterium tuberculosis with an MIC of 6.25 μg/mL. beta-Mangostin possesses in vitro antimalarial activity against Plasmodium falciparum, with an IC50 of 3.00 μg/mL. beta-Mangostin has potent anticancer activity against various cancers (such as hepatocellular carcinoma, leukaemic) .
Methylenetanshinquinone is a natural compound with antiplasmodial, antitrypanosomal and antioxidative activities. Methylenetanshinquinone can be used for the research of parasite infection .
Lactucin is an anti-inflammatory agent. Lactucin induces cancer cell apoptosis. Lactucin also shows analgesic, anticancer and antimalarial activities .
Lactucin (Standard) is the analytical standard of Lactucin. This product is intended for research and analytical applications. Lactucin is an anti-inflammatory agent. Lactucin induces cancer cell apoptosis. Lactucin also shows analgesic, anticancer and antimalarial activities [4].
Borrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor which is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei . Borrelidin is an inhibitor of Cdc28/Cln2 of the budding yeast, with an IC50 of 24 μM . Borrelidin is a potent angiogenesis inhibitor, with an IC50 of 0.8 nM. Borrelidin induces apoptosis in the tube-forming cells . Borrelidin has strong antimalarial activities, with IC50s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum, respectively .
ACKR1 is an atypical chemokine receptor that regulates chemokine levels and localization through high-affinity binding, induction of sequestration, degradation, or transcytosis. ACKR1, also known as a chemokine interceptor or decoy receptor, binds to chemokines such as CXCL11 and CXCL12/SDF1. ACKR1 Protein, Human (Cell-Free, His) is the recombinant human-derived ACKR1 protein, expressed by E. coli Cell-free , with N-10*His labeled tag.
Sulfadoxine-d3 is a deuterium labeled Sulfadoxine (HY-B0439). Sulfadoxine is a sulfonamide that is used, usually in combination with Pyrimethamine (HY-18062), for multidrug-resistant Plasmodium falciparum and P. vivax inhibition. Unlike PYR, Sulfadoxine has no impact on HIV replication or MT-2 cell cycle progression. But also Sulfadoxine exhibits suppression on respiratory, and urinary tract infections[1][2][3][4].
Primaquine-d3 (diphosphate) is the deuterium labeled Primaquine diphosphate. Primaquine Diphosphate (Primaquine phosphate), an 8-aminoquinoline, exerts a broad spectrum of activities against various stages of parasitic malaria. Primaquine Diphosphate remains as the only agent that destroys late hepatic stages and latent tissue forms of Plasmodium vivax and Plasmodium ovale[1][2].
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