DGK

Diacylglycerol kinase;

DGK (Diacylglycerol Kinase) modulates the balance between DAG and phosphatidic acid (PA). DGK phorylates DAG to generate PA. DGK has ten mammalian DGK subtypes (α-κ) with subtype-specific tissue distribution, and they can be classified into 5 types. Among them, DGKα and DGKζ specifically regulate the pool of DAG that is generated as a second messenger after stimulation of the T cell receptor. Whereas, DGKζ is the dominant isoform in T cells. Dysregulation of certain DGK isoforms leads to DAG-activation of PKC, attenuation of insulin signaling, and dysregulation of glucose metabolism. DGK plays a role in many physiological events, including cell proliferation and migration, glucose intake, immunity and neuronal network construction^[1]^[2]^[3].

References:

[1]. Riese MJ, et al. Diacylglycerol Kinases (DGKs): Novel Targets for Improving T Cell Activity in Cancer. Front Cell Dev Biol. 2016 Oct 17;4:108. [Content Brief]

[2]. Shirai Y, et al. Diacylglycerol kinase as a possible therapeutic target for neuronal diseases. J Biomed Sci. 2014 Apr 7;21(1):28. [Content Brief]

[3]. Massart J, et al. Role of Diacylglycerol Kinases in Glucose and Energy Homeostasis. Trends Endocrinol Metab. 2019 Sep;30(9):603-617. [Content Brief]

DGK Inhibitors (24)

DGK Related Products (25)
Antibodies (2)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-153343

BAY 2965501	Inhibitor	99.43%
BAY 2965501 is a potent and selective diacylglycerol kinase zeta (DGKζ) inhibitor. BAY 2965501 induces pERK activation. BAY 2965501 can be used for the research of cancer.

HY-153343A

(S)-BAY 2965501	Inhibitor	99.88%
(S)-BAY 2965501 is the left-handed isomer of BAY 2965501 (HY-153343). BAY 2965501 is a potent and selective diacylglycerol kinase zeta (DGKζ) inhibitor. BAY 2965501 induces pERK activation. BAY 2965501 can be used for the research of cancer.

HY-149874

BMS-502	Inhibitor	99.57%
BMS-502 (Compound 22) is a potent dual inhibitor of diacylglycerol kinase (DGK) α and ζ with IC₅₀ of 4.6 nM and 2.1 nM. BMS-502 enhanced T cell immune responses in mice. BMS-502 can be used in tumor immunity related research.

HY-135898

DGK-IN-1	Inhibitor	98.23%
DGK-IN-1 is a T cell activator extracted from patent WO2020006018A1, example 25. DGK-IN-1 can be used for tumor immunity.

HY-121638A

(5Z,2E)-CU-3	Inhibitor
(5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC₅₀ value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a K_m value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.

HY-159649

BMS-986408	Inhibitor

HY-149665

BMS-684	Inhibitor	99.76%
BMS-684 is a selective DGKα inhibitor with an IC₅₀ of 15 nM. BMS-684 inhibits DGKα kinase activity with >100-fold selectivity over the related DGK type I family members DGKβ and DGKγ. BMS-684 does not inhibit any of the other seven DGK isozymes.

HY-156569

DGKα-IN-2	Inhibitor	98.83%
DGKα-IN-2 (example 48) is a DGKα inhibitor with the IC₅₀ of 0.9 nM, extracted from patent WO2021105115. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-2 has the potential for cancer and immunology study.

HY-100960

Dioctanoylglycol	Inhibitor	≥98.0%
Dioctanoylglycol (Ethylene glycol dicaprylate), a diacylglycerol analog, is a diacylglycerol kinase (DGK) inhibitor (K_i of 58 μM).

HY-149667

BMS-332	Inhibitor	99.05%
BMS-332 is adualDGKα/ζlipid kinase inhibitor, with theIC₅₀of 0.005 (DGKα) and 0.001 μM (DGKζ).

HY-156567

AMB639752	Inhibitor	99.04%
AMB639752 is a potent DGKα inhibitor. AMB639752 restores restimulation induced cell death (RICD) in SAP deficient lymphocytes by inhibiting DGKα in intact cells. AMB639752 can be used for X-linked lymphoproliferative disease 1(XLP-1) research.

HY-149666

BMS-496	Inhibitor
BMS-496 is adualDGKα/ζlipid kinase inhibitor, with theIC₅₀of 0.09 (DGKα) and 0.006 μM (DGKζ).

HY-121638

CU-3	Inhibitor
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC₅₀ value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a K_m value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.

HY-156574

DGKζ-IN-4	Inhibitor
DGKζ-IN-4 is a DGK-zeta inhibitor. DGKζ-IN-4 can be used as an active component of pharmaceutical compositions. DGKζ-IN-4 is used to treat cancers associated with immune cell activation or cancers resistant to anti-PD-1 antibody/anti-PD-11 antibody treatment.

HY-153793

DGKζ-IN-1	Inhibitor
DGKζ-IN-1 (compound 9) is an inhibitor of DGKζ. DGKζ-IN-1 can be used for research in cancer related to immunocyte activation or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody.

HY-156578

DGKα-IN-8	Inhibitor
DGKα-IN-8 (Example 51) is a DGKα inhibitor (IC₅₀=22.491 nM; EC₅₀=0.256 nM). DGKα-IN-8 can be used to study cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection.

HY-156571

DGKα-IN-4	Inhibitor
DGKα-IN-4 (example 432) is a DGKα inhibitor with the IC₅₀ of 0.1 nM, extracted from patent WO2021105117. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-3 has the potential for cancer and immunology study.

HY-156570

DGKα-IN-3	Inhibitor
DGKα-IN-3 (example 25) is a DGKα inhibitor with the IC₅₀ of 283 nM, extracted from patent WO2021105115. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-2 has the potential for cancer and immunology study.

HY-122949

Momordicine I
Momordicine I, a triterpenoid compound extracted from momordica charantia L. Momordicine I alleviates isoproterenol-induced cardiomyocyte hypertrophy through suppression of PLA2G6 and DGK-ζ.

HY-160123

DGKζ-IN-5	Inhibitor
DGKζ-IN-5 is a DGKζ inhibitor (WO2023125681A1; compound A27a).

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DGK

DGK Related Products (25)

Antibodies (2)

DGK Related Products (25):