Diacylglycerol Kinase (DGK) regulates the equilibrium between phosphatidic acid (PA) and DAG. DAG is phorylated by DGK to produce PA. Ten mammalian DGK subtypes (-) that can be divided into five different types exist. Each subtype has its own tissue distribution. Among them, the production of DAG as a second messenger following stimulation of the T cell receptor is specifically regulated by DGK and DGK. However, in T cells, DGK is the predominant isoform. Certain DGK isoforms that are dysregulated cause DAG-activated PKC, attenuated insulin signaling, and dysregulated glucose metabolism. DGK participates in a variety of physiological processes, such as cell migration and proliferation, glucose uptake, immunity, and the development of neuronal networks.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V114696 | (1R)-BMS-986408 | 2618418-11-2 | (1R)-BMS-986408 is an orally effective dual DGK α/ζ inhibitor. |
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V32186 | (5Z,2E)-CU-3 | 1815598-71-0 | (5Z,2E)-CU-3is a novel, potent and selective diacylglycerol kinase alpha (DGKalpha) inhibitorwithanIC50valueof0.6 μM, attenuating cancer cell proliferation and simultaneously enhancing immune responses including anti-cancer immunity. |
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V109979 | AHL-7160 | AHL-7160 is a covalent DGKα inhibitor with dual functions: inhibiting enzyme activity (IC₅₀ ≈ 12 nM) and molecular glue-mediated degradation. | |
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V113321 | Alcudacigib TFA | Alcudacigib (compound 9) TFA is a DGKz inhibitor. | |
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V73996 | AMB639752 | 371210-26-3 | AMB639752 is a potent DGKα inhibitor. |
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V73987 | BAY 2965501 | 2732902-08-6 | BAY 2965501 is a potent and specific diacylglycerol kinase zeta (DGKζ) inhibitor. |
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V51059 | BAY-2965501 | DGKzeta inhibitor | |
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V74001 | BMS-332 | 2407892-15-1 | BMS-332 is a dual (bifunctional) inhibitor of DGKα/ζ lipokinase with IC50 of 0.005 μM (DGKα) and 0.001 μM (DGKζ) respectively. |
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V73995 | BMS-496 | 2407854-31-1 | BMS-496 is a dual (bifunctional) inhibitor of DGKα/ζ lipokinase with IC50 of 0.09 μM (DGKα) and 0.006 μM (DGKζ) respectively. |
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V73988 | BMS-502 | 2407854-18-4 | BMS-502 (Compound 22) is a potent dual (bifunctional) inhibitor of diacylglycerol kinase (DGK) α and ζ with IC50s of 4.6 nM and 2.1 nM. |
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V73997 | BMS-684 | 313552-29-3 | BMS-684 is a selective DGKα inhibitor (antagonist) with IC50 of 15 nM. |
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V99706 | BMS-986408 | 2618418-12-3 | BMS-986408 is an oral dual DGK α/ζ inhibitor that restores T cell-mediated anti-tumor immunity by enhancing T cell signaling. |
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V73999 | Cochlioquinone A (Luteoleersin) | 32450-25-2 | Cochlioquinone A is an ATP-competitive diacylglycerol kinase inhibitor (Ki= 3.1 μM). |
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V73989 | DGK-IN-1 | 2407892-34-4 | DGK-IN-1 is a T cell activator from patent WO2020006018A1, Example 25. |
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V116972 | DGK-IN-11 | 3023735-36-3 | DGK-IN-11 (compound 1) is a diacylglycerol kinase (DGK) inhibitor. |
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V117173 | DGK-IN-12 | 3023735-35-2 | DGK-IN-12 is a DGK inhibitor that can be used in cancer research. |
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V117149 | DGK-IN-13 | 3023735-55-6 | DGK-IN-13 is a DGK inhibitor that can be used in cancer research. |
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V104007 | DGK-IN-8 | 3039488-69-9 | DGK-IN-8 (Example 34) is a DGK inhibitor with IC50 ≤ 20 nM for DGKα and ζ. |
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V74000 | DGKα&ζ-IN-1 | 2830643-06-4 | DGKα&ζ-IN-1 (Compound II) is a DGK target inhibitor. |
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V117459 | DGKα&ζ-IN-2 | 3039488-61-1 | DGKα/ζ-IN-2 is a highly effective, orally active, and selective DGKα/ζ inhibitor with IC50 values of 23 nM (DGKα) and 1.2 nM (DGKζ). |