2. PI3K/Akt/mTOR Anti-infection
  3. PI4K Parasite
  4. 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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PI4Kβ-IN-1

PI4Kβ-IN-1 Chemical Structure

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PI4Kβ-IN-1 Related Antibodies

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Description

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[1].

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.

PI4Kβ-IN-1 Related Antibodies
In Vivo

PI4Kβ-IN-1 (Compound 18) (1-30 mg/kg, p.o., once daily, 4 consecutive days) demonstrates potent in vivo antimalarial efficacy in the humanized NOD-scid IL-2Rγnull (NSG) mouse model infected with Plasmodium falciparum Pf3D70087/N9[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 1, 3, 10, 30 mg/kg
Administration: p.o., once daily, 4 consecutive days
Result: Achieved an effective dose for 90% reduction in parasitemia (ED90) of 4.6 mg/kg.
Molecular Weight

374.44

Formula

C22H22N4O2
SMILES

O=C(N1C2CCOCC2)N(C)C3=C1C4=CC(C5=CC=CN=C5C)=CC=C4N=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PI4Kβ-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PI4Kβ-IN-1PI4KParasitePhosphatidylinositol 4 kinasesPI4 kinasesmalariaPlasmodium falciparumPI4KβInhibitorinhibitorinhibit

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