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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 .
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) .
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) .
DSM1465 (Compound 82) is a potent, selective inhibitor of P. falciparum dihydroorotate dehydrogenase (PfDHODH) with an IC50 value of 15 nM, inhibits P. falciparum 3D7 (Pf3D7) parasites with an EC50 value of 1.4 nM. DSM1465 shows potent in vivo activity in the humanized P. falciparum mouse model .
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 .
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 .
(-)-Halofantrine ((-)-SKF-102886 free base; (-)-WR-171669) is an inhibitor of the malignant malaria parasite (P. falciparum) and targets multidrug-resistant P. falciparum. The pharmacokinetic parameters of (-)-Halofantrine in rats vary depending on the route of administration, distinguishing it from other isomers .
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 .
CCOE-5 is a chalcone compound with antiplasmodial activity, showing an IC50 of 1.4 μg/mL against P. falciparum (3D7), and an IC50 of less than 5 μg/mL against P. falciparum (INDO). CCOE-5 holds promise for research in the field of anti-infective therapies .
DXR-IN-1 (Compound 13E) is an inhibitor of 1-deoxy-D-ketose 5-phosphate reductoisomerase (DXR). DXR-IN-1 is highly selective for P. falciparum DXR (IC50=0.030 μM). DXR-IN-1 inhibits the growth of P. falciparum by binding to the active site of DXR and blocking its catalytic activity .
Pyronaridine is an orally active Mannich base anti-malarial agent. Pyronaridine is active against P. falciparum and Echinococcus granulosus infection .
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 .
Antimalarial agent 46 (Compound 42a) is an antimalarial agent with antimalarial activity. Antimalarial agent 46 shows inhibitory activity against P. falciparum lines .
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 .
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 .
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 .
NEU-1017 is a broad-spectrum antiparasitic agent. NEU-1017 inhibits T. brucei, L. major, and P. falciparum with EC50 values of 210 nM, 240 nM, and 3 nM, respectively .
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Ambelline is an alkaloid that can be isolated from the Amaryllidaceae family. Ambelline shows antimalarial activity against Dd2 P. falciparum strain, with an IC50 of 7.3 ± 0.3 μM .
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) .
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 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 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 .
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 .
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 .
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 .
Villalstonine is a bisindole alkaloid with various biological activities including anticancer, antimalarial, and antiamoebic activities. Villalstonine exhibits potent antiplasmodial activity against the multidrug-resistant K1 strain of P. falciparum with an IC50 value of 0.27 μM .
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) .
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 .
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) .
Pyronaridine (tetraphosphate) (Standard) is the analytical standard of Pyronaridine (tetraphosphate). This product is intended for research and analytical applications. Pyronaridine tetraphosphate is an orally active Mannich base anti-malarial agent. Pyronaridine tetraphosphate is active against P. falciparum and Echinococcus granulosus infection .
MED6-189, a kalihinol analog, disrupts apicoplast function and vesicular trafficking in P. falciparum malaria (IC50 < 50 nM). MED6-189 targets the apicoplast, a nonphotosynthetic plastid found in most Apicomplexa parasites that is crucial for the synthesis of isoprenoids .
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].
SPB07935 inhibits the plasmepsin II in Plasmodium falciparum and can be used as an antimalarial agent. SPB07935 regulates the life cycle of P. falciparum, inhibits the growth of Plasmodium strains FcB1 and 3D7 with IC50 of 8 μM and 4.7 μM .
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 .
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 .
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 .
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 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 .
Beauvericin A is a cyclodepsipeptide and derivative of beauvericin originally isolated from B. bassiana that has diverse biological activities. It is active against M. tuberculosis (MIC=25 μg/mL) and P. falciparum (IC50=12 μg/mL).2 Beauvericin A is toxic to brine shrimp (LD100=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 .
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 .
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 .
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 .
Quassin (Standard) is the analytical standard of Quassin. This product is intended for research and analytical applications. 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 .
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 .
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 .
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 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) .
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 .
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 .
GSK932121 is an antimalarial drug with activity that inhibits the electron transport chain of P. falciparum. GSK932121 acts selectively on this pathogen at the level of cytochrome bc1 (complex III). The synthesis method of GSK932121 is highly efficient, and the final structure can be obtained in only 5 steps. The synthesis of GSK932121 can be prepared atKilog scale to support clinical studies .
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 .
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 .
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) .
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) .
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 .
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 .
Emoquine-1 is an orally active and potent antimalarial drug. Emoquine-1 is efficient against multidrug-resistant Plasmodium parasites, including the Artemisinin-resistant quiescent stage. Emoquine-1 is active against proliferative P. falciparum with IC50 values of 20-55 nM. Emoquine-1 is a candidate to fight Plasmodium parasites resistant to artemisinin-based combination therapies (ACTs) with a capacity to eliminate persistent parasites .
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) .
DHFR-IN-20 (Compound LA1) is a Plasmodium falciparumdihydrofolate 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 .
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 .
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 .
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 .
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 .
PfCLK3-IN-1 (Compound 4) is a covalent inhibitor for Plasmodium falciparumCLK3 (Pf CLK3) under alkaline conditions with an pEC50 of 7.1. PfCLK3-IN-1 reduces mature gametocytes in sexual stage parasites, and prevents transmission. PfCLK3-IN-1 inhibits P. falciparum Dd2-B2 clone with an IC50 of 239.5 nM .
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.
Fosmidomycin is an orally active antibiotic, which exhibits antimalarial activity through inhibition of 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DOXP reductoisomerase). Fosmidomycin inhibits P. falciparum strains 3D7, HB3, Dd2 and A2, with IC50s of 150, 71, 170 and 150 ng/mL, respectively. Fosmidomycin exhibits synergistic effect with Clindamycin (HY-B1455), and ameliorates malaria in mouse model .
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 .
DXR-IN-4 (Compound 12a) is the inhibitor for 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR). DXR-IN-4 inhibits DXR in Plasmodium falciparum Pf DXR, Escherichia coli Ec DXR, and Mycobacterium tuberculosis Mt DXR with IC50s of 18, 4.9 and 89 nM, respectively. DXR-IN-4 exhibits antimalarial activity that inhibits P. falciparum strains 3D7 and Dd2 with IC50 of 11 μM and 12 μM .
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 .
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 .
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 .
(Rac)-ACT-451840 is an isomer of ACT-451840 that exhibits significant antimalarial effects. (Rac)-ACT-451840 exhibits significant antimalarial activity against P. berghei-infected mice at a dose of 20 mg/kg (ED90=13 mg/kg), and has an inhibitory effect at a dose of 300 mg/kg. The ED90 of (Rac)-ACT-451840 in the P. falciparum humanized immunodeficient mouse model is 3.7 mg/kg. (Rac)-ACT-451840 is similar to artemisinin, with a rapid onset of action but requires repeated high doses.
Steffimycin B is an anthracycline bacterial metabolite originally isolated from Streptomyces. It binds to DNA, preferentially intercalating at sites containing cytosine and guanine.2 Steffimycin B is cytotoxic to MCF-7, KB, NCI-H187, and Vero cells (IC50s=3.5, 6.75, 3.28, and 10.5 μM, respectively). It is active against M. tuberculosis (MIC=5.2 nM), B. cereus (MIC=1.56 μg/mL), and P. falciparum (IC50=2.19 μM).
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 .
Melicopine is an alkaloid found in Z. simulans with antimalarial and anticancer activities. It exhibits inhibitory activity against chloroquine-sensitive 3D7 and chloroquine-resistant Dd2 strains of P. falciparum, with IC50 values of 29.7 and 33.7 µg/mL, respectively. Melicopine is cytotoxic to prostate cancer cells PC-3M and LNCaP (IC50 values of 47.9 and 37.8 µg/mL), but has no effect on non-cancerous HEK293 cells (IC50 greater than 100 µg/mL). Melicopine holds promise for research in anticancer and anti-infection fields .
Pyrocoll is a bacterial metabolite originally isolated from Streptomyces. It inhibits the growth of A. aurescens, A. globiformis, A. oxydans, A. pascens, and R. erythropolis bacteria (MICs=10, 1, 10, 3, and 10 μg/mL, respectively) and HMO2, HepG2, and MCF-7 cancer cells (GI50s=0.28, 0.42, and 2.2 μg/mL, respectively) in vitro. Pyrocoll is also active against P. falciparum and T. rhodesiense (IC50s=1.19 and 1.97 μg/mL, respectively).
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 .
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 .
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 .
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 .
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) .
Diacetylcercosporin is a perylenequinone produced by Cercospora and Septoria that has diverse biological activities. Diacetylcercosporin inhibits the growth of P. falciparum strains that are sensitive and resistant to chloroquine (IC50s=2.75 and 1.94 μM for D6 and W2 clones, respectively) and L. donovani parasites (IC50=3.1 μM) in vitro. Diacetylcercosporin exhibits cytotoxicity against SK-MEL, KB, BT549, and SKOV3 human cancer cell lines (IC50s=4.8-8.7 μM). Diacetylcercosporin is also a phytotoxin that inhibits the growth of lettuce and bentgrass at a concentration of 1.62 mM.
Takinib (Standard) is the analytical standard of Takinib. This product is intended for research and analytical applications. 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)[1][2][3].
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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
HDAC-IN-88 (Compound HJ-9) is the inhibitor for HDAC that inhibits HDAC6, HDAC1, HDAC2, HDAC8 and HDAC3 with IC50s of 0.226, 1.103, 2.308, 3.255 and 3.864 μM, respectively. HDAC-IN-88 inhibits the proliferation of cancer cell HepG2, HCT116 and MV4-11 with IC50 of 5.47, 9.78 and 0.38 μM, inhibits the migration of HCT116, arrests the cell cycle at G0/G1 phase, and induces apoptosis and autophagy in MV4-11. HDAC-IN-88 reduces ROS level and mitochondrial membrane potential. HDAC-IN-88 exhibits antimalarial activity that inhibits P. falciparum 3D7 with EC50 of 165 nM. HDAC-IN-88 also exhibits anti-angiogenic activity .
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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions 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 .
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 .
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 .
Villalstonine is a bisindole alkaloid with various biological activities including anticancer, antimalarial, and antiamoebic activities. Villalstonine exhibits potent antiplasmodial activity against the multidrug-resistant K1 strain of P. falciparum with an IC50 value of 0.27 μM .
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) .
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 .
Quassin (Standard) is the analytical standard of Quassin. This product is intended for research and analytical applications. 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 .
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 .
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) .
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) .
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) .
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 .
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.
Fosmidomycin is an orally active antibiotic, which exhibits antimalarial activity through inhibition of 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DOXP reductoisomerase). Fosmidomycin inhibits P. falciparum strains 3D7, HB3, Dd2 and A2, with IC50s of 150, 71, 170 and 150 ng/mL, respectively. Fosmidomycin exhibits synergistic effect with Clindamycin (HY-B1455), and ameliorates malaria in mouse model .
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 .
Melicopine is an alkaloid found in Z. simulans with antimalarial and anticancer activities. It exhibits inhibitory activity against chloroquine-sensitive 3D7 and chloroquine-resistant Dd2 strains of P. falciparum, with IC50 values of 29.7 and 33.7 µg/mL, respectively. Melicopine is cytotoxic to prostate cancer cells PC-3M and LNCaP (IC50 values of 47.9 and 37.8 µg/mL), but has no effect on non-cancerous HEK293 cells (IC50 greater than 100 µg/mL). Melicopine holds promise for research in anticancer and anti-infection fields .
The pfHPRT (Plasmodium falciparum hypoxanthine-guanine phosphoribosyltransferase) protein is a member of the LDH/MDH (lactate dehydrogenase/malate dehydrogenase) superfamily. It plays a crucial role in the purine metabolism salvage pathway of the malaria-causing parasite Plasmodium falciparum. PfLDH Protein, P. falciparum (His) is the recombinant PfLDH protein, expressed by E. coli , with C-His labeled tag.
The pfHPRT (Plasmodium falciparum hypoxanthine-guanine phosphoribosyltransferase) protein is a member of the LDH/MDH (lactate dehydrogenase/malate dehydrogenase) superfamily. It plays a crucial role in the purine metabolism salvage pathway of the malaria-causing parasite Plasmodium falciparum. pfHPRT Protein, P. falciparum (His) is the recombinant pfHPRT protein, expressed by E. coli , with N-His labeled tag.
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].
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. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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