DGKα&ζ-IN-2 

DGKα/ζ-IN-2 is a potent, orally active and selective dual DGKα/ζ inhibitor with IC₅₀ values of 23 nM (DGKα) and 1.2 nM (DGKζ). DGKα/ζ-IN-2 exhibits selectivity over other DGK isoforms, such as DGKβ and DGKγ. DGKα/ζ-IN-2 shows robust and dose-dependent immune activation in the presence of antigen presentation in an OT-1 murine model. DGKα/ζ-IN-2 can be used for antitumor immunity^[1].

DGKα/ζ-IN-2 (compound 17) 对多种激酶 (HPK1、EPHA2、FLT3、KDR、KIT、PDGFRβ 和 TRKA) 表现出优异的选择性，IC₅₀ 值 > 10 μM^[1]。
DGKα/ζ-IN-2 在 Jurkat 细胞 (EC₅₀ = 64 nM) 和人全血 (EC₅₀ = 447 nM) 中均能有效促进 IL-2 的产生，显示出强大的功能活性^[1]。
DGKα/ζ-IN-2 表现出均衡的体外 ADME 特性，具有低的人体微粒体清除率 (0.6 L/h/kg)、高的 Caco-2 渗透性 (1.2 × 10⁻⁶ cm/s)，以及在禁食状态模拟肠液 (> 1000 μg/mL) 和模拟胃液 (659 μg/mL) 中均具有高溶解度^[1]。

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

DGKα/ζ-IN-2 (5、25 和 50 mg/kg，口服，单次给药) 在 OT-I 小鼠模型中，在抗原呈递的情况下，可诱导强烈的、剂量依赖性的 CD8⁺ T 细胞活化^[1]。

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

646.68

C₃₅H₃₄F₄N₆O₂

3039488-61-1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Xiang M, et al. Discovery of Fluoroalkenes as Dual Inhibitors of Diacylglycerol Kinases Alpha and Zeta (DGKα/ζ). J Med Chem. 2025 Oct 9;68(19):20789-20813.  [Content Brief]