dgk

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.

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.

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.

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

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

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.

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].

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].

Hodgkinsine is a pyrrolidinoindoline alkaloid that has been found inP. colorataand has analgesic activity.1It increases latency to paw licking in the hot plate test and latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 5 mg kg. 1.Amador, T.A., Verotta, L., Nunes, D.S., et al.Antinociceptive profile of hodgkinsinePlanta Med.66(8)770-772(2000)

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-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.

Hodgkinsine B is an alkaloid and isomer of hodgkinsine that has analgesic activity.1It increases the latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 10 mg kg. 1.Kodanko, J.J., Hiebert, S., Peterson, E.A., et al.Synthesis of all low-energy stereoisomers of the tris(pyrrolidinoindoline) alkaloid hodgkinsine and preliminary assessment of their antinociceptive activityJ. Org. Chem.72(21)7909-7914(2007)

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-5, also known as compound A27a (WO2023125681A1), is an inhibitor of DGKζ [1].

DGKζ-IN-1 (compound 9) is a DGKζ inhibitor with potential applications in cancer research, particularly for studying immunocyte activation and resistance to anti-PD-1 anti-PD-L1 antibody therapies [1].

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

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-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.

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.

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].

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