PfPK6-IN-1 

PfPK6-IN-1 is a potent and selective PfPK6 inhibitor with an IC₅₀ of 0.3 μM. PfPK6-IN-1 inhibits hemozoin formation, a Plasmodium-specific pathway with IC₅₀ of 13 μM against β-hematin (βH). PfPK6-IN-1 exhibits rapid and broad-spectrum anti-malarial properties, being effective against both chloroquine-sensitive and resistant strains.PfPK6-IN-1 can be used for the study of antimalarial^[1].

PfPK6-IN-1 (Compound 12) exhibits EC₅₀s of 116 nM against Dd2 asexual blood stage parasites and 210 nM against the P. falciparum 3D7 strain^[1].
PfPK6-IN-1 (48 h) is a fast-acting compound active throughout the asexual blood cycle and clears 99.9% of the parasites (99.9% PCT) within 32.5 h^[1].
PfPK6-IN-1 activity is unchanged after PfPK6 knockdown (EC₅₀ of 129 nM in the physiological PK6 levels versus 153 nM in the knockdown) in the Dd2^{PK6 cKD} line^[1].
PfPK6-IN-1 (20-850 nM, 13 months) resists the drug resistance of chloroquine resistant P. falciparum Dd2-B2 strain by targeting the digestive vesicle transport proteins (PfCRT and PfMDR1) of the malaria parasite ^[1].
PfPK6-IN-1 (0-500 nM, 72 h) interaction with chloroquine is antagonistic in 3D7 but synergistic in Dd2^[1].
PfPK6-IN-1 (0-32 h) inhibits hemozoin formation by directly inhibiting the formation of β-hematin in P. falciparum 3D7, and increasing the accumulation of toxic hemoglobin in 3D7 parasites^[1].
PfPK6-IN-1 (0-72 h) is active against Cambodian and Ugandan P. falciparum isolates^[1].

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

PfPK6-IN-1 (Compound 12) (15-50 mg/kg, i.v. or i.p., single dose or once daily for 4 days) completely prevents mice from being infected with P. berghei, and partially inhibits the existing infection of P. berghei in mice^[1].

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

650.74

C₃₄H₄₁F₃N₈O₂

2417648-94-1

CN1CCC(C(NC2=CC(OC3=CC=C4C(N(C)C(NC5=CC=C(CN6CCN(CC)CC6)C(C(F)(F)F)=C5)=N4)=C3)=CC=N2)=O)CC1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Nardella F, et al. Plasmodiumfalciparum protein kinase 6 and hemozoin formation are inhibited by a type II human kinase inhibitor exhibiting antimalarial activity. Cell Chem Biol. 2025 Jul 17;32(7):926-941.e23.  [Content Brief]