dgk

(5Z,2E)-CU-3 is a potent and highly selective inhibitor of the DGKα isozyme with an IC50 value of 0.6 μM, competing with ATP and exhibiting a Km value of 0.48 mM. It specifically targets the catalytic region of DGKα without affecting the regulatory region and has demonstrated antitumor and immunogenic effects by promoting cancer cell apoptosis and T cell activation.

R 59-022 (DKGI-I) is a diacylglycerol kinase (DGK) inhibitor and a 5-HT Receptor antagonist that blocks filovirus internalization in host cells. R 59-022 activates protein kinase C (PKC), inhibits intestinal smooth muscle contractility, and enhances O2- production induced by 1-oleoyl-2-acetylglycerol.

Dioctanoylglycol (ethane-1,2-diyl dioctanoate) is a diacylglycerol kinase inhibitor.

R59949 is used as a Diacylglycerol kinase (DGK) inhibitor.

R 59-022 hydrochloride (DKGI-I hydrochloride) is a 5-HT Receptor antagonist that activates protein kinase C (PKC).R 59-022 hydrochloride is a DGK inhibitor (IC50:2.8 µM) that inhibits the phosphorylation of OAG to OAPA.R 59-022 enhances thrombin-induced triglyceride production in platelets and inhibits the production of phosphatidic acid in neutrophils. R 59-022 enhances thrombin-induced diglyceride production in platelets and inhibits phosphatidic acid production in neutrophils.

BAY 2965501 is a potent and selective diacylglycerol kinase zeta (DGKζ) inhibitor that induces pERK activation, and it can be utilized in cancer research.

BMS-684 is a selective and potent DGKα inhibitor (IC50: 15 nM) with potential antitumor activity.BMS-684 inhibits DGKα kinase, DGKβ, and DGKγ.BMS-684 activates T-cells, which may prevent and treat immune-related diseases.

BMS-502 is a potent dual inhibitor of diacylglycerol kinase (DGK) α and ζ that induces immune responses in human and mouse T cells and blocks intracellular checkpoint signaling in T cells. BMS-502 stimulates immune responses in a dose-dependent manner and can be used to study immune-related diseases.

DGK-IN-8 (Example 34) is a DGK inhibitor with IC50 values of ≤ 20 nM for both DGKα and ζ. It is applicable in cancer research.

DGK-IN-9 (Compound 15) is an orally active and selective inhibitor of DGKζ with an IC50 of 6.1 nM. It is capable of activating IL-2 expression in Jurkat-IL2 nanoluc cells with an EC50 of 153 nM. DGK-IN-9 is applicable in tumor research.

DGK-IN-12 is a DGK inhibitor useful for cancer research.

DGK-IN-11 (Compound 1) is an inhibitor of diacylglycerol kinase (DGK). It exhibits inhibitory activity against DGKα and DGKγ. DGK-IN-11 regulates intracellular diacylglycerol levels and enhances T cell activation, cytokine production, and proliferation. This compound is applicable in cancer research.

DGK-IN-13 is a DGK inhibitor that can be utilized in cancer research.

DGK-IN-1, an extracted T cell activator, holds potential in leveraging tumor immunity.

DGKα/ζ-IN-2 is a potent, orally active, and highly selective inhibitor of DGKα/ζ, exhibiting IC50 values of 23 nM for DGKα and 1.2 nM for DGKζ. It shows excellent selectivity over other DGK isoforms such as DGKβ and DGKγ. In the OT-1 mouse model, DGKα/ζ-IN-2 demonstrates significant and dose-dependent immune activation under antigen-presenting conditions. This compound can be utilized in research related to anti-tumor immunity.

DGKα&ζ-IN-1 (Compound II) is a DGK inhibitor that enhances T-cell function and synergistically interacts with PD-1, providing therapeutic advantages in immune and tumor contexts [1].

DGKζ-IN-4, a DGK-zeta inhibitor, is utilized as an active ingredient in pharmaceutical formulations to treat cancers associated with immune cell activation or those resistant to anti-PD-1/anti-PD-L1 antibody treatments [1].

DGKζ-IN-3 is an inhibitor of diacylglycerol kinase zeta (DGK-ζ), employed in the treatment of both liquid and solid cancers, as well as other diseases regulated by DGK-ζ [1].

DGKζ-IN-7 (compound 97) is an orally active inhibitor of DGKζ, exhibiting an IC50 of 33.4 nM. It hinders the secretion of IL-2 and is applicable in the research of cancer and autoimmune diseases.

DGKζ-IN-6 (compound 40) is an orally active inhibitor of DGKζ with an IC50 value of 45.5 nM. It inhibits the secretion of IL-2 and is useful for research into cancer and autoimmune diseases.

DGKζ-IN-10 (compound 349) is an inhibitor of DGKζ, demonstrating an IC50 of ≤200 nM.

DGKα-IN-9 (example 298) is an inhibitor of DGKα.

DGKζ-IN-9 (compound 73) is an inhibitor of DGKζ with an IC50 value of ≤200 nM.

DGKα-IN-10 is a potent, orally active DGKα inhibitor with an IC50 of 0.27 nM. It can induce IL-2 release and T cell proliferation, making it useful for cancer research, including studies on colon cancer.