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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 .
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 .
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) .
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 .
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 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) .
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 .
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) .
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 .
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 .
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-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 .
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 .
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 .
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 .
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 .
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) .
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 .
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 .
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 .
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 .
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 .
P-orlandin, a fungal metabolite, prevents FREP1 from binding to gametocytes or ookinetes. P-orlandin effectively inhibits P. falciparum infection in mosquitoes .
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 .
Pyronaridine is an orally active Mannich base anti-malarial agent. Pyronaridine is active against P. falciparum and Echinococcus granulosus infection .
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 .
Pyronaridine tetraphosphate is an orally active Mannich base anti-malarial agent. Pyronaridine tetraphosphate is active against P. falciparum and Echinococcus granulosus infection .
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 .
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 .
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 .
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 .
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 .
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) .
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 .
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 .
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) .
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 .
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 .
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 .
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 .
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 .
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 .
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].
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 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 .
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 .
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 .
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 .
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 .
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.
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 .
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 .
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 .
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].
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 .
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 .
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) .
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.
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.
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 .
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) .
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 .
P-orlandin, a fungal metabolite, prevents FREP1 from binding to gametocytes or ookinetes. P-orlandin effectively inhibits P. falciparum infection in mosquitoes .
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) .
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 .
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 .
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 .
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.
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 .
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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