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Halofantrine hydrochloride (SKF-102886 hydrochloride; WR-171669 hydrochloride) is a blocker that delays the delayed rectifier potassium current by inhibiting human ERG channels, and it is a potent antimalarial agent with oral activity. Halofantrine hydrochloride inhibits the Cap1-dependent oxidative stress response of Candida albicans, suppresses ROS responses, and enhances the antifungal (Fungal) activity of oxidative damage agents. Halofantrine hydrochloride exhibits antifungal activity in the Galleria mellonella model, and shows antimalarial activity against Plasmodium strains both in vitro and in animal models. Halofantrine hydrochloride can be used in studies related to invasive candidiasis, falciparum malaria, and vivax malaria .
Halofantrine (SKF-102886 hydrochloride; WR-171669 hydrochloride) is a blocker that delays the delayed rectifier potassium current by inhibiting human ERG channels, and it is a potent antimalarial agent with oral activity. Halofantrine inhibits the Cap1-dependent oxidative stress response of Candida albicans, suppresses ROS responses, and enhances the antifungal (Fungal) activity of oxidative damage agents. Halofantrine exhibits antifungal activity in the Galleria mellonella model, and shows antimalarial activity against Plasmodium strains both in vitro and in animal models. Halofantrine can be used in studies related to invasive candidiasis, falciparum malaria, and vivax malaria .
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 .
MMV1557817 is an orally active and potent antimalarial compound. MMV1557817 is a selective, nanomolar inhibitor of both Plasmodium falciparum and Plasmodiumvivax aminopeptidases M1 and M17, leading to inhibition of end-stage hemoglobin digestion in asexual parasites .
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 .
PI4K-IN-3 (Compound 27) is an orally active PI4K inhibitor with an IC50 of 1.9 nM for Plasmodiumvivax PI4K. PI4K-IN-3 has no hERG channel inhibition and mammalian cytotoxicity. PI4K-IN-3 has significant selectivity against the human MINK1 and MAP4K4 kinases but with low selectivity against human PI3Kα and PI4Kβ. PI4K-IN-3 has potent antimalarial activity and significantly reduces parasitaemia in NSG mice mouse models of Plasmodium falciparum malaria .
MMV688533 is an antimalarial agent. MMV688533 interferes with intracellular trafficking, lipid utilization, and endocytosis pathways in Plasmodium falciparum. MMV688533 rapidly kills asexual blood-stage Plasmodium falciparum and Plasmodiumvivax parasites in vitro and reduces parasitemia in a Plasmodium falciparum NSG mouse model. MMV688533 can be used for the research of malaria .
Purine phosphoribosyltransferase-IN-2 is a potent inhibitor of the Plasmodium falciparum ((Pf)), Plasmodiumvivax ((Pv)) and Trypanosoma brucei ((Tbr)) 6-oxopurine phosphoribosyltransferase (PRT), with Kis of 30, 20 and 2 nM, respectively .
D44 is a PlasmodiumFKBP35 inhibitor that selectively inhibits the FKBD35PPIase activity, with PPIaseIC50 values of 132 nM and 125 nM for Plasmodium falciparum and Plasmodiumvivax, respectively. D44 exhibits antiplasmodium activity and can be used in research related to infectious diseases .
NIC is a host invasion inhibitor. NIC can suppress host invasion by interacting with the major invasion-related protein, merozoite surface protein 1 (MSP-1). NIC prevents the invasion of Plasmodium falciparum and Plasmodiumvivax into the host .
RO-09-4609 exhibits antimicrobial activity, that inhibits Candida albicans, Trypanosoma brucei and Plasmodiumvivax through inhibition of N-myristoyl transferase .
Arterolane (OZ 277) (maleate) is an orally active antimalarial. Arterolane exhibits potent activity against erythrocytic stages of P. falciparum and Plasmodiumvivax. Arterolane (maleate) is promising for research of falciparum malaria .
Primaquine-d3 (diphosphate) is the deuterium labeled Primaquine diphosphate. Primaquine Diphosphate (Primaquine phosphate), an 8-aminoquinoline, exerts a broad spectrum of activities against various stages of parasitic malaria. Primaquine Diphosphate remains as the only agent that destroys late hepatic stages and latent tissue forms of Plasmodiumvivax and Plasmodium ovale .
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 .
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 .
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 .
(S)-DSM1465 is a Plasmodiumdihydroorotate dehydrogenase (DHODH) inhibitor. (S)-DSM1465 exhibits potential inhibitory activity against Plasmodium falciparum and Plasmodiumvivax, and can be used in malaria research .
Halofantrine hydrochloride (Standard) is the analytical standard of Halofantrine hydrochloride. This product is intended for research and analytical applications. Halofantrine hydrochloride (SKF-102886 hydrochloride; WR-171669 hydrochloride) is a blocker that delays the delayed rectifier potassium current by inhibiting human ERG channels, and it is a potent antimalarial agent. Halofantrine hydrochloride inhibits the Cap1-dependent oxidative stress response of Candida albicans, suppresses ROS responses, and enhances the antifungal (Fungal) activity of oxidative damage agents. Halofantrine hydrochloride exhibits antifungal activity in the Galleria mellonella model, and shows antimalarial activity against Plasmodium strains both in vitro and in animal models. Halofantrine hydrochloride can be used in studies related to invasive candidiasis, falciparum malaria, and vivax malaria.
Isopentaquine is an orally active antimalarial agent. Isopentaquine induces mild morphological changes in the exoerythrocytic stage of Plasmodium fallax, with a ED50 of 6.7 mg/L. Isopentaquine causes degenerative changes in the development of Plasmodium oocysts in infected mosquitoes. Isopentaquine reduces the infectivity of Plasmodium falciparum gametocytes. Isopentaquine impairs sympathetic cardiovascular reflexes. Isopentaquine decreases the recurrence rate and total disease duration of Plasmodiumvivax infection. Isopentaquine can be used in malaria-related research .
Antimalarial agent 55 is an orally potent inhibitor of PfA-M1 and PfA-M17 aminopeptidases from Plasmodium falciparum, with Ki values of 27 nM and 81 nM, respectively. Antimalarial agent 55 exhibits potent nanomolar activity against homologous enzymes from Plasmodiumvivax and Plasmodium berghei, with Ki values of 2 nM, 4 nM, 190 nM and 18 nM for Pv-M1, Pb-M1, Pv-M17 and Pb-M17, respectively. Antimalarial agent 55 possesses significant antiplasmodial activity, as well as cross-species inhibitory capacity and broad-spectrum activity that is unaffected by existing drug resistance mechanisms. Antimalarial agent 55 can be used in malaria research .
KAI-407 is an orally active inhibitor of PlasmodiumPI4K kinase, which can broadly inhibit multiple stages of the parasite lifecycle. KAI-407 exhibits EC50s of for the blood stage of malignant Plasmodium of 81 nM; for the liver schizonts of P. yoelii of 88 nM; and IC50s for the liver schizonts and dormant bodies of P. cynomolgi of 0.64 μM and 0.69 μM respectively. KAI-407 can prevent Plasmodium berghei infection 100%. KAI-407 can be used for the study of vivax malaria .
IMP-1002 is a PlasmodiumN-myristoyltransferase (NMT) inhibitor. IMP-1002 inhibits myristoylation activity, blocks parasite development. IMP-1002 can be used for the research of malaria .
WR 30090 (Compound 37) is a broad-spectrum antimalarial agent that does not rely on the classical antifolate pathway. WR 30090 exhibits strong activity against a variety of chloroquine-sensitive and resistant Plasmodium falciparum strains, especially the highly resistant Vietnamese strain. WR 30090 shows high activity in mouse malaria tests, with a minimum effective dose of 5 mg/kg and a minimum cure dose of 20 mg/kg. WR 30090 can be used for research on acute malaria .
NSC-80141 is a Kinesin-5 inhibitor. NSC-80141 exerts selective inhibitory activity against human kinesin-5 (HsEg5) (IC50: 9.4 μM), while shows weak inhibitory activity against Plasmodium kinesin-5 (PvEg5) (IC50: 27.3 μM). NSC-80141 serves as a tool compound for distinguishing human and Plasmodium homologous proteins .
Etoprine is a potent orally active dihydrofolate reductase (DHFR) inhibitor. Etoprine competitively inhibits testicular DHFR to disrupt tetrahydrofolate and DNA synthesis in rapidly dividing cells. Etoprine acts as an antifertility agent in male mice and reduces fecundity in male rats .
MMV693183 is an orally active inhibitor of Plasmodium falciparumacetyl-CoA synthetase (AcAS), with an IC50 of 300 nM against Plasmodium falciparum. MMV693183 exhibits potent inhibitory activity against clinical isolates of malaria parasites, including Artemisinin (HY-B0094)-resistant strains. MMV693183 is metabolized in vivo into the active antimetabolite CoA-MMV693183, which exerts effects of killing asexual blood-stage parasites and blocking transmission to Anopheles mosquitoes by binding to and inhibiting the function of acetyl-CoA synthetase, thereby reducing the levels of acetyl-CoA and 4'-phosphopantetheine. In humanized mouse models, MMV693183 shows favorable in vivo efficacy, drug-like properties, and no significant cytotoxicity or off-target activity against human cells. MMV693183 is widely used in malaria-related research as a parasiticide and metabolic disruptor .
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 .
ACKR3 is an atypical chemokine receptor that regulates chemokine levels and localization through high-affinity binding, induction of sequestration, degradation, or transcytosis. ACKR3, also known as a chemokine interceptor or decoy receptor, binds to chemokines such as CXCL11 and CXCL12/SDF1. ACKR1 Protein, Human (Cell-Free, His) is the recombinant human-derived ACKR1 protein, expressed by E. coli Cell-free , with N-10*His labeled tag.
Sulfadoxine-d3 is a deuterium labeled Sulfadoxine (HY-B0439). Sulfadoxine is a sulfonamide that is used, usually in combination with Pyrimethamine(HY-18062), for multidrug-resistant Plasmodium falciparum and P. vivax inhibition. Unlike PYR, Sulfadoxine has no impact on HIV replication or MT-2 cell cycle progression. But also Sulfadoxine exhibits suppression on respiratory, and urinary tract infections .
Primaquine-d3 (diphosphate) is the deuterium labeled Primaquine diphosphate. Primaquine Diphosphate (Primaquine phosphate), an 8-aminoquinoline, exerts a broad spectrum of activities against various stages of parasitic malaria. Primaquine Diphosphate remains as the only agent that destroys late hepatic stages and latent tissue forms of Plasmodiumvivax and Plasmodium ovale .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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