dgkα

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

DGKα-IN-2 (example 48), a potent DGKα inhibitor with an IC50 of 0.9 nM, significantly enhances the anti-tumor efficacy of anti-PD-1 therapy by amplifying T cell proliferation and function, making it a valuable agent for cancer and immunological research.

DGKα-IN-3 (example 25), with an IC50 of 283 nM, is a selective DGKα inhibitor that enhances anti-PD-1's anti-tumor activity by promoting T cell proliferation and function, highlighting its potential for cancer and immunology research applications.

DGKα-IN-4 (example 432) is an inhibitor of DGKα with an IC50 value of 0.1 nM. This compound notably potentiates the anti-tumor efficacy of anti-PD-1 therapy by augmenting T cell proliferation and function and shows promise for research in cancer and immunology.

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].

DGKα-IN-6, a diacylglycerol kinase alpha (DGKα) inhibitor characterized by an inhibitory concentration (IC50) of 1.377 nM,holds promise for use in cancer research.

DGKα-IN-7 is a potent DGKα inhibitor with an IC50 value of 6.225 nM and potential applications in cancer research.

DGKα-IN-8 (Example 51), a potent diacylglycerol kinase alpha (DGKα) inhibitor, exhibits an IC50 of 22.491 nM and an EC50 of 0.256 nM. It is applicable in cancer research, particularly for solid tumors, and in studies of viral infections such as HIV and hepatitis B virus [1].

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.

(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.

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.

JNJ-3790339 is an analogue of Ritanserin, a selective and potent diacylglycerol kinase (DGKα) inhibitor (IC50: 9.6 μM) that upregulates T-cell activation and induces toxic effects on malignant cells.

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.

AMB639752 is a potent inhibitor of diacylglycerol kinase alpha (DGKα) that reinstates restimulation-induced cell death (RICD) in SAP-deficient lymphocytes through DGKα inhibition within intact cells. This compound is applicable in the research of X-linked lymphoproliferative disease 1 (XLP-1) [1].

BMS-496 is a dual DGKα ζ lipid kinase inhibitor exhibiting IC50 values of 0.09 μM (DGKα) and 0.006 μM (DGKζ) [1].

BMS-332 is a dual inhibitor of the lipid kinases DGKα and DGKζ, demonstrating half-maximal inhibitory concentrations (IC50) of 0.005 μM for DGKα and 0.001 μM for DGKζ [1].