dgk-α

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.

(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.

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

Procarbazine hydrochloride (NSC-77213 HCl) is the hydrochloride salt of a methylhydrazine derivative with antineoplastic and mutagenic activities. Although the exact mode of cytotoxicity has not been elucidated, procarbazine, after metabolic activation, appears to inhibit the trans-methylation of methionine into transfer RNA (t-RNA), thereby preventing protein synthesis and consequently DNA and RNA synthesis. This agent may also undergo auto-oxidation, resulting in the formation of cytotoxic free radicals which damage DNA through an alkylation reaction.

PNU-159682, a metabolite of anthracycline nemorubicin, is a DNA topoisomerase II inhibitor with excellent cytotoxicity.

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.

Hodgkinsinetrimethyl (iodide) is the trimethyl iodide derivative of Hodgkinsine. Hodgkinsine functions as an opioid receptor agonist and NMDA receptor antagonist, offering analgesic and antihyperalgesic effects. Additionally, Hodgkinsine exhibits antiviral, antibacterial, and antifungal activities.

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)

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)

IRAK4-IN-7 (CA-4948) is a selective and potent IRAK4 kinase inhibitor with in vivo activity in a TLR4-induced cytokine release model.

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.