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^[1].

PI4Kβ-IN-1 (Compound 18) 在存在 ATP 的情况下强效抑制重组 Plasmodium vivax 磷脂酰肌醇 4-激酶 IIIβ (PvPI4K)，其 IC₅₀ 值为 1.2 nM^[1]。
PI4Kβ-IN-1 (96 h) 对 Plasmodium falciparum 无性血期 (ABS) 寄生虫表现出强效抗疟活性，其 IC₅₀ 值分别为 0.024 μM (NF54，药物敏感株) 和 0.053 μM (K1，多药耐药株)^[1]。
PI4Kβ-IN-1 对 Plasmodium falciparum 配子体具有杀灭活性，其 IC₅₀ 值分别为 0.38 μM (未成熟配子体) 和 0.61 μM (晚期配子体)^[1]。
PI4Kβ-IN-1 抑制 Plasmodium falciparum 肝裂殖体 (IC₅₀ = 0.065 μM)，并阻断 Plasmodium falciparum 配子形成 (IC₅₀ = 0.87 μM)^[1]。
PI4Kβ-IN-1 对哺乳动物细胞表现出低细胞毒性，其 IC₅₀ 值分别为 30 μM (CHO 细胞)、18.2 μM (HepG2 细胞) 和 47.8 μM (L6 细胞)^[1]。
PI4Kβ-IN-1 抑制人共济失调-毛细血管扩张突变体激酶 (HsATM)，其 IC₅₀ 值分别为 2 nM (10 μM ATP) 和 103 nM (500 μM ATP)^[1]。

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

PI4Kβ-IN-1 (Compound 18) (1-30 mg/kg，口服，每日一次，连续 4 天) 在感染 Plasmodium falciparum Pf3D7⁰⁰⁸⁷/N9 的人源化 NOD-scid IL-2Rγnull (NSG) 小鼠模型中表现出强效的体内抗疟活性^[1]。

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

374.44

C₂₂H₂₂N₄O₂

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

• [1]. Dziwornu GA, et al. Novel Inhibitors of Plasmodium Phosphatidylinositol 4-kinase IIIβ with Low Propensity for Resistance: Life Cycle Stage Activity and In Vivo Efficacy in a Humanized Mouse Malaria Infection Model. J Med Chem. 2025 Aug 28;68(16):17736-17751.  [Content Brief]