2. PI3K/Akt/mTOR
  3. PI4K PI3K
  4. CHMFL-PI4K-127

CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy.

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CHMFL-PI4K-127 Chemical Structure

CHMFL-PI4K-127 Chemical Structure

CAS No. : 2377604-81-2

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CHMFL-PI4K-127 Related Antibodies

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Description

CHMFL-PI4K-127 (compound 15g) is an orally active, potent and high selective PfPI4K (Plasmodium falciparum PI4K kinase) inhibitor, with an IC50 of 0.9 nM. CHMFL-PI4K-127 exhibits potent activity against 3D7 Plasmodium falciparum, with an EC50 of 25.1 nM. CHMFL-PI4K-127 shows antimalaria efficacy[1].

IC50 & Target

PI4K

0.9 ± 0.1 nM (IC50)

PI3Kδ

104 ± 3 nM (IC50)

PI3Kα

191 ± 36 nM (IC50)

PI3Kγ

324 ± 19 nM (IC50)

PI3Kβ

392 ± 27 nM (IC50)

Vps34

681 ± 25 nM (IC50)

In Vitro

CHMFL-PI4K-127 (compound 15g) displays high selectivity against PfPI4K over human lipid and protein kinase[1].
CHMFL-PI4K-127 exhibits EC50 values of 23–47 nM against a panel of the drug-resistant strains of P. falciparum[1].

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

CHMFL-PI4K-127 Related Antibodies
In Vivo

CHMFL-PI4K-127 (compound 15g) (Orally; 0-80 mg/kg/day for 7 days; 0-15 mg/kg, once) exhibits the antimalaria efficacy in both blood stage (80 mg/kg) and liver stage (1 mg/kg) of Plasmodium in infected rodent model[1].

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

Animal Model: Balb/c mice were infected by P. yoelii[1].
Dosage: 0, 60, 80 mg/kg
Administration: Orally, daily for 7 days
Result: Displayed significant in vivo antimalarial activities in a dose-dependent manner and 80 mg/kg × 7 days treatment generated curative effects. The 60 mg/kg dosage resulted in suppressive effects during the drug treatment but relapsed after stopping treatment.
Animal Model: Balb/c mice were infected by P. yoelii[1].
Dosage: 0, 1, 5, 15 mg/kg
Administration: Orally, once
Result: Provided the full protection and cure at 1 mg/kg with no negligible parasite visible in the liver of all tested mice at 24, 48, 72, 96, 144 and 196 h, indicating true causal prophylactic efficacy.
Molecular Weight

402.85

Formula

C18H15ClN4O3S
CAS No.
SMILES

O=C(C1=CN=CC(C2=CC(NS(=O)(C3=CC=CC=C3)=O)=C(Cl)N=C2)=C1)NC
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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CHMFL-PI4K-127 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:

CHMFL-PI4K-1272377604-81-2PI4KPI3KPhosphatidylinositol 4 kinasesPI4 kinasesPhosphoinositide 3-kinasePI4K kinaseKinase inhibitorMalariaBlood stageLiver stageantimalariaInhibitorinhibitorinhibit

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