PI4Kβ-IN-1
PI4Kβ-IN-1 is an orally active and selective PI4Kβ inhibitor, with an IC50 of 0.9 nM. PI4Kβ-IN-1 exhibits inhibitory activity against all stages of the P. falciparum life cycle, including blood, liver, and transmission stages. PI4Kβ-IN-1 demonstrates potent antimalarial efficacy in the mouse model infected with Plasmodium falciparum. PI4Kβ-IN-1 can be used for the study of malaria caused by Plasmodium falciparum.
For research use only. We do not sell to patients.
- Formula: C22H22N4O2
- Molecular Weight:374.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Parasite Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
PI4KB 0.9 nM (IC50) |
In Vitro
PI4Kβ-IN-1 (Compound 18) potently inhibits recombinant Plasmodium vivax phosphatidylinositol 4-kinase IIIβ (PvPI4K) with an IC50 value of 1.2 nM in the presence of ATP[1].
PI4Kβ-IN-1 (96 h) exhibits potent antiplasmodial activity against Plasmodium falciparum asexual blood stage (ABS) parasites, with IC50 values of 0.024 μM (NF54, drug-sensitive strain) and 0.053 μM (K1, multidrug-resistant strain), respectively[1].
PI4Kβ-IN-1 shows gametocytocidal activity against Plasmodium falciparum gametocytes, with IC50 values of 0.38 μM (immature gametocytes) and 0.61 μM (late-stage gametocytes), respectively[1].
inhibits Plasmodium falciparum liver schizonts (IC50 = 0.065 μM) and blocks Plasmodium falciparum gamete formation (IC50 = 0.87 μM)[1].
PI4Kβ-IN-1 exhibits low cytotoxicity against mammalian cells, with IC50 values of 30 μM (CHO cells), 18.2 μM (HepG2 cells), and 47.8 μM (L6 cells), respectively[1].
PI4Kβ-IN-1 inhibits human ataxia-telangiectasia-mutated (HsATM) kinase with IC50 values of 2 nM (10 μM ATP) and 103 nM (500 μM ATP), respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Plasmodium falciparum Pf3D70087/N9 parasites were intravenously or intraperitoneally administered to 6-week-old (or relevant age) immunodeficient NOD-scid IL-2Rγnull (NSG) mice to construct the humanized mouse malaria infection model[1]
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Dosage:1, 3, 10, 30 mg/kg
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Administration:p.o., once daily, 4 consecutive days
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Result:Achieved an effective dose for 90% reduction in parasitemia (ED90) of 4.6 mg/kg.
Chemical Information
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Molecular Weight 374.44
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Formula C22H22N4O2
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SMILES
O=C(N1C2CCOCC2)N(C)C3=C1C4=CC(C5=CC=CN=C5C)=CC=C4N=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)