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.
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- Formel: C22H22N4O2
- Molecular Weight:374.44
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
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PI4KB 0.9 nM (IC50) |
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.
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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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
PI4Kβ-IN-1 Related Classifications
HY-175732 Related Classifications
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