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) demonstrates an excellent selectivity across a broad panel of kinases (HPK1, EPHA2, FLT3, KDR, KIT, PDGFRβ and TRKA), with IC₅₀ values > 10 μM^[1].
DGKα/ζ-IN-2 demonstrates potent functional activity by promoting IL-2 production in both Jurkat cells (EC₅₀ = 64 nM) and human whole blood (EC₅₀ = 447 nM)^[1].
DGKα/ζ-IN-2 exhibits a balanced in vitro ADME profile, with low human microsomal clearance (0.6 L/h/kg), high Caco-2 permeability (1.2 × 10⁻⁶ cm/s), and high solubility in both fasted-state simulated intestinal fluid (> 1000 μg/mL) and simulated gastric fluid (659 μg/mL)^[1].

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

DGKα/ζ-IN-2 (5, 25, and 50 mg/kg, p.o., single dose) induces robust, dose-dependent CD8⁺ T cell activation in the presence of antigen presentation in an OT-I murine model^[1].

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

646.68

C₃₅H₃₄F₄N₆O₂

3039488-61-1

F/C(C1=NC(C2=CC=NN=C2)=CN=C1)=C\C3=CC=C(C(C(F)(F)F)=C3N4CCOC5(C4)CCN(CC5)CC6CC6)OC7=CC=CC=C7

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.