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WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains (including Pyrimethamine (HY-18062)-resistant P. falciparum strains) as well as T. gondii .
13,21-Dihydroeurycomanone, a natural compound isolated from Eurycoma longifolia root, possesses anti-parasite activity for Plasmodium falciparum and Toxoplasma gondii .
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 .
Antimalarial agent 13 (Compound 1) is a potent antimalarial agent. Antimalarial agent 13 shows inhibition with EC50 values of 124 nM and 2.5 μM against P. falciparum parasite and HepG2, respectively .
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 .
WR99210 hydrochloride is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 hydrochloride shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains as well as T. gondii .
Antimalarial agent 16 (Compound 4h) is a parasite inhibitor. Antimalarial agent 16 shows antimalarial activity, and can inhibit P. falciparum parasite growth (IC50=2.0 nM) .
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 .
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 .
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) .
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 .
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 .
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 .
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 .
Antimalarial agent 8 (Compound 7e) is a novel orally active class of antimalarials. Antimalarial agent 8 is potent in vitro against P. falciparum and is orally efficacious (40 mg/kg) in an in vivo mouse model of malaria .
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 .
6-Methylhydroxyyangolensate is a limonoid can be extracted from Khaya grandifoliola. 6-Methylhydroxyyangolensate has low antimalarial activity in vitro, with an IC50 of 21.59 μg/ml against P. falciparum (W2/Indochina clone) .
Antimalarial agent 18 is an potent antimalarial agent, based on electronic, highly lipophilic and siderophoric properties. Antimalarial agent 18 belongs to acyloxymethyl series, as a fosmidomycin surrogate, which is potent IspC inhibitor against the non-mevalonate isoprenoid biosynthesis pathway. Antimalarial agent 18 inhibits P. falciparum (IC50=50 nM) and A. baumanii (IC50=390 nM) .
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 .
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) .
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 .
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 .
Antimalarial agent 19 (compound 6e) is an antimalarial active agent. Antimalarial agent 19 has antimalarial activity for the blood stage of P. falciparum K1 and P. berghei with EC50 values of 0.3 µM, 15.3 µM, respectively. Antimalarial agent 19 has good aqueous solubility, intestinal permeability and microsomal stability compared to gamhepathiopine .
Antimalarial agent 26 is an orally active 1,4-naphthoquinones derivative with antimalarial activities. Antimalarial agent 26 shows cytotoxicity against P. falciparum and selectivity over mammalian cell lines. Antimalarial agent 26 inhibits P. burghei induced parasitemia in vivo .
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 .
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 .
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 .
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 .
SR9186 (ML368) is a potent CYP3A4 inhibitor with IC50 s for inhibition of midazolam → 1′hydroxymidazolam, testosterone → 6β-hydroxytestosterone, and vincristine → vincristine M1 of 9, 4, and 38 nM, respectively. SR-9186 inhibits liver-stage development of P. falciparum to block ivermectin metabolism .
Psicofuramine a nucleoside antibiotic and has the inhibition of xanthosine 5'-phosphate aminase. Psicofuranine also specifically inhibits GMP synthase, and interrupts parasite growth. Psicofuranine exhibits a dose-dependent inhibition of P. falciparum growth .
SARS-CoV-IN-1 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-1 shows anti-Coronavirus activity with an EC50 of 4.9 μM in Vero cells. SARS-CoV-IN-1 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 15.4 and 133.2 nM; and IC90s of 25.7 and 459.1 nM; respectively. Antimalarial and antiviral activities .
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 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 .
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) .
SARS-CoV-IN-3 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-3 shows anti-Coronavirus activity with an EC50 of 3.6 μM in Vero cells. SARS-CoV-IN-3 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 11.7 and 20.4 nM; and IC90s of 29.19 and 56 nM; respectively. SARS-CoV-IN-3 reduces HIV-1-induced cytopathic effect with an EC50 of 10 μM in MT-4 cells .
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 .
SARS-CoV-IN-2 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-2 shows anti-Coronavirus activity with an EC50 of 1.9 μM in Vero cells. SARS-CoV-IN-2 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 21.5 and 30 nM; and IC90s of 51.0 and 99.9 nM; respectively. SARS-CoV-IN-2 reduces HIV-1-induced cytopathic effect with an EC50 of 2.9 μM in MT-4 cells. Antimalarial and Antiviral Activities .
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 .
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 .
Antimalarial agent 12 (compound R-3b) is a potent antimalarial agent. Antimalarial agent 12 shows growth inhibition on P. falciparum Dd2 Strain (EC50=155 nM), 3D7 strain (EC50=136 nM). Antimalarial agent 12 has CC50 values of 10,000 to 50,000 nM for HEK-293 and hPHep cell lines. Antimalarial agent 12 has a MIC of >250,000 nM for Escherichia coli .
Asperaculane B is a fungal metabolite against P. falciparum transmission with an IC50 of 7.89 µM. Asperaculane B also inhibits the development of asexual P. falciparum with IC50 of 3 µM, and it is nontoxic to human cells .
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 .
Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor CDK, with IC50s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity for CDK over a range of other protein kinases (IC50>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum .
Pulixin prevents FREP1 from binding to P. falciparum-infected cell lysate. Pulixin blocks the transmission of the parasite to mosquitoes with an EC50 of 11 µM. Pulixin also inhibits the proliferation of asexual-stage P. falciparum with an EC50 of 47 nM .
MMV008138 is a species-selective IspD (enzyme 2-C-methyl-d-erythritol 4-phosphate cytidylyltransferase)-targeting antimalarial agent, with an IC50 of 44 nM for PfIspD (P. falciparum IspD). MMV008138 inhibits the growth of P. falciparum Dd2 strain with an IC50 of 250 nM .
Primaquine diphosphate is a potent antimalaria agent and a potent gametocytocide in falciparum malaria. Primaquine diphosphate prevents relapse in vivax and ovale malaria .
Isochondrodendrine ( Isochondrodendrin) is a class of bisbenzylisoquinoline alkaloid isolated from Isolona ghesquiereina. Isochondodendrine has strong antiplasmodial activity against Plasmodium falciparum .
Pyronaridine is an orally active Mannich base anti-malarial agent. Pyronaridine is active against P. falciparum and Echinococcus granulosus infection .
trans-Cinnamic anhydride is a Parasite inhibitor tnat can be isolated from Cinnamomum zeylanicum and exhibits moderate activity against Plasmodium falciparum .
Pyronaridine tetraphosphate is an orally active Mannich base anti-malarial agent. Pyronaridine tetraphosphate is active against P. falciparum and Echinococcus granulosus infection .
P-orlandin, a fungal metabolite, prevents FREP1 from binding to gametocytes or ookinetes. P-orlandin effectively inhibits P. falciparum infection in mosquitoes .
Naphthoquine phosphate is a potent and orally active antimalarial agent. Naphthoquine phosphate has thorough killing function for various schizonts of plasmodia, including resistance of P. falciparum to Chloroquine .
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 .
Artemisone (Artemifone) is a potent and semi-synthetic antimalarial, inhibits P. falciparum strains, with a mean IC50 of 0.83 nM . Artemisone is also a potent inhibitor of human CMV .
Halofantrine (SKF-102886 free base) is a highly lipophilic antimalarial active against Chloroquine-resistant strains of Plasmodium falciparum . Halofantrine blocks HERG potassium channels .
Desmethyl ferroquine (SSR97213) is the active and major metabolite of Ferroquine. Ferroquine is an antimalarial. Desmethyl ferroquine shows significant activity against Chloroquine-susceptible and resistant P. falciparum strains .
SpdSyn binder-1 is a weak binder, which binds in the active site of plasmodium falciparumspermidine synthase. SpdSyn binder-1 can be used for the research of malaria .
Antimalarial agent 20 (Compound 49c) is an antimalarial agent with an IC50 of 0.6 nM against P. falciparum NF54 parasite strain in the NF54 albumax assay .
9-Hydroxycalabaxanthone (Xanthone I) is a known xanthone isolated from Garcinia mangostana Linn. 9-Hydroxycalabaxanthone has quorum-sensing inhibitory, anti-microbial, and anti-malarial activities (IC50=1.2-1.5 µM) .
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 .
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 .
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 .
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 .
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) .
Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits P. falciparum with an IC50 of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity .
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 .
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 .
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 .
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 .
Anti-infective agent 7 is a potent anti-infectious agent. Anti-infective agent 7 has anti-infection activity against P. falciparum (IC50=2.5 μM) and M. tuberculosis (MIC=9 μM) .
Pyronaridine-d4 (tetraphosphate) is the deuterium labeled Pyronaridine tetraphosphate[1]. Pyronaridine tetraphosphate is an orally active Mannich base anti-malarial agent. Pyronaridine tetraphosphate is active against P. falciparum and Echinococcus granulosus infection[2][3].
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 .
MMV665916, a quinazolinedione derivative, is an antimalarial agent. MMV665916 displays antiplasmodial activity against P. falciparum FcB1 strain with EC50 value of 0.4 µM and presents the high selectivity index (SI>250) .
Koshidacin B is an antiplasmodial cyclic tetrapeptide with antiplasmodial activity against P. falciparum FCR3 and K1 strain with IC50 values of 0.89 and 0.83 μM, respectively. Koshidacin B suppresses malaria parasites in vivo, it can be used for the research of parasites infection .
Antimalarial agent 28 (Compound 2i) is an antiplasmodial agent. Antimalarial agent 28 inhibits P. berghei, with IC50s of 0.561 μM, 0.14 μM, 4.34 μM for Liver stage, early gametocytes and ring stages of P. falciparum .
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) .
Antimalarial agent 24 (Compound 7) is an antimalarial agent in vitro. Antimalarial agent 24 inhibits P. falciparum W2 strain with an IC50 of 0.81 μM. Antimalarial agent 24 displays a CC50 higher than 200 μM against HepG2 cells .
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 .
Anti-infective agent 3 (compound 3l) shows antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC50 values of 0.47 and 0.13 μM, respectively. Anti-infective agent 3 shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 4 μg/mL .
Anti-infective agent 2 (compound 3k) shows antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC50 values of 0.07 and 2.20 μM, respectively. Anti-infective agent 2 shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 32 μg/mL .
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 .
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 .
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 .
Cabamiquine (DDD107498) succinate 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 succinate inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2 .
6-O-Methacrylate, a trilobolide, is isolated from the leaves of Wedelia trilobata. 6-O-Methacrylate displays marked antimalarial activity, with IC50 of 8.9 μg/mL against P. falciparum parasite. 6-O-Methacrylate also has anti-tobacco mosaic virus (TMV) activity .
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 .
HSP90-IN-21 (5e) is an antiplasmodial agent, with IC50 values of 0.04, 0.17 and 2.91 μM against erythrocytic stage of P. falciparum (Pf3D7 and PfDd2 strains), cytotoxicity of human liver hepatocellular carcinoma cell line (HepG2), respectively .
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 .
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 .
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 (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 .
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 .
Anti-infective agent 1 (compound 3a) is a potent and selective antiprotozoal and antimycobacterial agent. Anti-infective agent 1 shows antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC50 values of 10.95 and 0.06 μM, respectively. Anti-infective agent 1 shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 8 μg/mL .
Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM . Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM .
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) .
TPE-MI (Tetraphenylethene maleimide) is a thiol probe for measuring unfolded protein load and proteostasis in cells. TPE-MI can report imbalances in proteostasis in induced pluripotent stem cell models of Huntington disease, as well as cells transfected with mutant Huntington exon 1 before the formation of visible aggregates. TPE-MI also detects protein damage following dihydroartemisinin research of the malaria parasitesPlasmodium falciparum .
Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity .
Desethyl chloroquine diphosphate is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine diphosphate possesses antiplasmodic activity .
Antimalarial agent 14 (Compound N3) is a potent inhibitor of mitochondrial electron transport. Antimalarial agent 14 can serve as an anti-malarial agent .
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 .
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].
Orotidine 5'-monophosphate trisodium is a pyrimidine nucleotide. Orotidine 5'-monophosphate trisodium is synthesized via the de novo synthesis pathway for DNA synthesis in a large number of microorganisms including M. tuberculosis, S. cerevisiae, S. typhimurium and P. falciparum to name a few. The synthesis of orotidine 5'-monophosphate trisodium uses phosphoribosyl pyrophosphate (PRPP) and orotic acid (OA) as the substrates catalyzed by orotate phosphoribosyltransferase (OPRT) .
Anti-infective agent 6 (compound 28) is a potent anti-infectious agent. Anti-infective agent 6 shows a good activity against P. falciparum F32-ART (IC50=1.4 μM) with a good selectivity index (SI>36). Anti-infective agent 6 also shows a potency against L. donovani (IC50=3.5 μM) .
Isochamaejasmin is a biflavonoid with anti-cancer, antiplasmodial and insecticidal activities. Isochamaejasmin displays a potent NF-κB (NF-κB) activation activity. Isochamaejasmin could cause DNA damage and induce apoptosis via the mitochondrial pathway in AW1 cells . Isochamaejasmin also has a moderate antiplasmodial activity (IC50 of 7.3 μM for P. falciparum) and relatively low cytotoxicity (CC50 of 29.0 μM) .
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 .
Atovaquone-d5 is the deuterium labeled Atovaquone. 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[1][2].
Radicicol is an inhibitor of Hsp90 with an IC50 value < 1 μM, and leads to proteasomal degradation . Radicicol exhibits inhibition on PDK with IC50s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparumtopoisomerase VIB . Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC50 value of 16.04 μM .
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 .
cis-Atovaquone-d4 is deuterium labeled Atovaquone. 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[1][2].
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) .
Dehydrocorydaline (13-Methylpalmatine) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP . Dehydrocorydaline elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities . Dehydrocorydaline shows strong anti-malarial effects (IC50=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain .
ELQ-300 is a potent and orally bioavailable antimalarial agent, acts as an inhibitor of the reductive (Qi) site of the cytochrome bc1 complex (cyt bc1). ELQ-300 inhibits growth of P. falciparum Dd2, Tm90-C2B, and D1 with IC50 values of 6.6, 4.6 and 160 nM, respectively. ELQ-300 can be used for the research of antimalarial .
Dehydrocorydaline (13-Methylpalmatine) hydroxyl is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline hydroxyl elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities. Dehydrocorydaline hydroxyl shows strong anti-malarial effects (IC50=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
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 .
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) .
Plm IV inhibitor-1 (compound 6) is a potent plasmepsin IV (Plm IV) inhibitor with IC50s of 4.1, 0.80, 0.25, 0.35 µM for Plm I, Plm II, Plm IV, Cat D, respectively .
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.
Lactucin is an anti-inflammatory agent. Lactucin induces cancer cell apoptosis. Lactucin also shows analgesic, anticancer and antimalarial activities .
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 .
7-Chloro-4-(piperazin-1-yl)quinolone is an important scaffold in medicinal chemistry. 7-Chloro-4-(piperazin-1-yl)quinolone is a potent sirtuin inhibitor and also inhibits the serotonin uptake (IC50 of 50 μM). 7-Chloro-4-(piperazin-1-yl)quinolone exhibits antimalarial activity on D10 and K1 strains of P. falciparum with IC50s of 1.18 μM and 0.97 μM, respectively .
Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
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 .
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 .
Biotin-C1-PEG3-C3-amido-C5-Gly-Arg-Gly-N3 TFA is used for detection of modification site for N-myristoylated and GPI-anchored proteins in blood-stage P. falciparum . Biotin-C1-PEG3-C3-amido-C5-Gly-Arg-Gly-N3 (TFA) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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 .
Jatrorrhizine is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities . Jatrorrhizine is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE . Jatrorrhizine reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters .
Jatrorrhizine chloride is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities . Jatrorrhizine chloride is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE . Jatrorrhizine chloride reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters .
Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities . Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE . Jatrorrhizine hydroxide reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters .
Antitrypanosomal agent 9 (compound 1) is a potent antitrypanosomal agent. Antitrypanosomal agent 9 shows inhibitory activity against T. b. brucei, with an IC50 of 1.15 μM. Antitrypanosomal agent 9 can be used for human African trypanosomiasis (HAT) research .
TPE-MI (Tetraphenylethene maleimide) is a thiol probe for measuring unfolded protein load and proteostasis in cells. TPE-MI can report imbalances in proteostasis in induced pluripotent stem cell models of Huntington disease, as well as cells transfected with mutant Huntington exon 1 before the formation of visible aggregates. TPE-MI also detects protein damage following dihydroartemisinin research of the malaria parasitesPlasmodium falciparum .
Biotin-C1-PEG3-C3-amido-C5-Gly-Arg-Gly-N3 TFA is used for detection of modification site for N-myristoylated and GPI-anchored proteins in blood-stage P. falciparum . Biotin-C1-PEG3-C3-amido-C5-Gly-Arg-Gly-N3 (TFA) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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) .
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 .
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.)
13,21-Dihydroeurycomanone, a natural compound isolated from Eurycoma longifolia root, possesses anti-parasite activity for Plasmodium falciparum and Toxoplasma gondii .
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 .
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 .
6-Methylhydroxyyangolensate is a limonoid can be extracted from Khaya grandifoliola. 6-Methylhydroxyyangolensate has low antimalarial activity in vitro, with an IC50 of 21.59 μg/ml against P. falciparum (W2/Indochina clone) .
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 .
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 .
Asperaculane B is a fungal metabolite against P. falciparum transmission with an IC50 of 7.89 µM. Asperaculane B also inhibits the development of asexual P. falciparum with IC50 of 3 µM, and it is nontoxic to human cells .
Pulixin prevents FREP1 from binding to P. falciparum-infected cell lysate. Pulixin blocks the transmission of the parasite to mosquitoes with an EC50 of 11 µM. Pulixin also inhibits the proliferation of asexual-stage P. falciparum with an EC50 of 47 nM .
Isochondrodendrine ( Isochondrodendrin) is a class of bisbenzylisoquinoline alkaloid isolated from Isolona ghesquiereina. Isochondodendrine has strong antiplasmodial activity against Plasmodium falciparum .
trans-Cinnamic anhydride is a Parasite inhibitor tnat can be isolated from Cinnamomum zeylanicum and exhibits moderate activity against Plasmodium falciparum .
P-orlandin, a fungal metabolite, prevents FREP1 from binding to gametocytes or ookinetes. P-orlandin effectively inhibits P. falciparum infection in mosquitoes .
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 .
Koshidacin B is an antiplasmodial cyclic tetrapeptide with antiplasmodial activity against P. falciparum FCR3 and K1 strain with IC50 values of 0.89 and 0.83 μM, respectively. Koshidacin B suppresses malaria parasites in vivo, it can be used for the research of parasites infection .
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) .
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 .
6-O-Methacrylate, a trilobolide, is isolated from the leaves of Wedelia trilobata. 6-O-Methacrylate displays marked antimalarial activity, with IC50 of 8.9 μg/mL against P. falciparum parasite. 6-O-Methacrylate also has anti-tobacco mosaic virus (TMV) activity .
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 .
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 .
Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM . Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM .
Orotidine 5'-monophosphate trisodium is a pyrimidine nucleotide. Orotidine 5'-monophosphate trisodium is synthesized via the de novo synthesis pathway for DNA synthesis in a large number of microorganisms including M. tuberculosis, S. cerevisiae, S. typhimurium and P. falciparum to name a few. The synthesis of orotidine 5'-monophosphate trisodium uses phosphoribosyl pyrophosphate (PRPP) and orotic acid (OA) as the substrates catalyzed by orotate phosphoribosyltransferase (OPRT) .
Isochamaejasmin is a biflavonoid with anti-cancer, antiplasmodial and insecticidal activities. Isochamaejasmin displays a potent NF-κB (NF-κB) activation activity. Isochamaejasmin could cause DNA damage and induce apoptosis via the mitochondrial pathway in AW1 cells . Isochamaejasmin also has a moderate antiplasmodial activity (IC50 of 7.3 μM for P. falciparum) and relatively low cytotoxicity (CC50 of 29.0 μM) .
Radicicol is an inhibitor of Hsp90 with an IC50 value < 1 μM, and leads to proteasomal degradation . Radicicol exhibits inhibition on PDK with IC50s of 230 μM (PDK1) and 400 μM (PDK3). Radicicol is an antifungal and antimalarial antibiotic, impairs mitochondrial replication by targeting P. falciparumtopoisomerase VIB . Radicicol is also an inhibitor of fat mass and obesity-associated protein (FTO), with an IC50 value of 16.04 μM .
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) .
Dehydrocorydaline (13-Methylpalmatine) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP . Dehydrocorydaline elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities . Dehydrocorydaline shows strong anti-malarial effects (IC50=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain .
Dehydrocorydaline (13-Methylpalmatine) hydroxyl is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline hydroxyl elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities. Dehydrocorydaline hydroxyl shows strong anti-malarial effects (IC50=38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
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 .
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 .
Jatrorrhizine is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities . Jatrorrhizine is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE . Jatrorrhizine reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters .
Jatrorrhizine chloride is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities . Jatrorrhizine chloride is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE . Jatrorrhizine chloride reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters .
Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities . Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE . Jatrorrhizine hydroxide reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters .
pfHPRT Protein, part of the LDH/MDH superfamily, is specified. PfLDH Protein, P. falciparum (His) is the recombinant PfLDH protein, expressed by E. coli, with C-His labeled tag. The total length of PfLDH Protein, P. falciparum (His) is 316 a.a., with molecular weight of ~34.9 KDa.
pfHPRT Protein, part of the LDH/MDH superfamily, is specified. pfHPRT Protein, P. falciparum (His) is the recombinant pfHPRT protein, expressed by E. coli, with N-His labeled tag. The total length of pfHPRT Protein, P. falciparum (His) is 231 a.a., with molecular weight of ~28.6 kDa.
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].
Pyronaridine-d4 (tetraphosphate) is the deuterium labeled Pyronaridine tetraphosphate[1]. Pyronaridine tetraphosphate is an orally active Mannich base anti-malarial agent. Pyronaridine tetraphosphate is active against P. falciparum and Echinococcus granulosus infection[2][3].
Atovaquone-d5 is the deuterium labeled Atovaquone. 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[1][2].
cis-Atovaquone-d4 is deuterium labeled Atovaquone. 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[1][2].
Biotin-C1-PEG3-C3-amido-C5-Gly-Arg-Gly-N3 TFA is used for detection of modification site for N-myristoylated and GPI-anchored proteins in blood-stage P. falciparum . Biotin-C1-PEG3-C3-amido-C5-Gly-Arg-Gly-N3 (TFA) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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