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 Related Products (45)
Antibodies (2)

By Effects:	Inhibitors (44) Substrate (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-153343

Veludacigib	Inhibitor	99.92%
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	99.31%
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-149665

BMS-684	Inhibitor	98.52%
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-159649

BMS-986408	Inhibitor	99.35%
BMS-986408 is an orally active inhibitor of DGKα and DGKζ, with IC₅₀ values of 0.0003 μM and 0.002 μM, respectively. BMS-986408 activates intratumoral T cell responses, enhances the priming and expansion of tumor-reactive T cells in tumor-draining lymph nodes, and functions as an immunostimulant. BMS-986408 can be used in the research of tumors.

HY-121638A

(5Z,2E)-CU-3	Inhibitor
(5Z,2E)-CU-3 is an isomer of CU-3 (HY-121638). CU-3 is a DGKα inhibitor with an IC₅₀ of 0.6 μM. CU-3 competitively reduces DGKα’s affinity for ATP via binding to the enzyme’s catalytic region. CU-3 induces apoptosis in cancer cells. CU-3 promotes T-cell activation and enhances IL-2 production. CU-3 can be used for the research of hepatocellular carcinoma and cervical cancer.

HY-153793A

Alcudacigib TFA	Inhibitor	99.72%
Alcudacigib (ASP1570; DGKζ-IN-1) TFA is an orally active diacylglycerol kinase ζ (DGKζ) inhibitor, with an IC₅₀ of 4.7 nM against human DGKζ and an IC₅₀ of 3.0 nM against mouse DGKζ. Alcudacigib TFA selectively inhibits the kinase activity of DGKζ and induces proteasome-dependent degradation of DGKζ protein. Alcudacigib TFA enhances the anti-tumor functions of T cells and NK cells. Alcudacigib TFA can be used for the research of advanced/metastatic solid tumors.

HY-159649A

(1R)-BMS-986408	Inhibitor	99.03%
(1R)-BMS-986408 is an orally active dual DGK α/ζ inhibitor that restores T cell-mediated anti-tumor immunity by enhancing T cell signaling.

HY-177107

DGK-IN-10	Inhibitor
DGK-IN-10 (example 61) is a DGK inhibitor with IC₅₀ values of ≤ 10 nM for both DGKα and DGKζ. DGK-IN-10 can be used for the research of diseases including cancer.

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 a dual DGKα/ζ lipid kinase inhibitor, with IC₅₀s of 5 and 1 nM against DGKα and DGKζ, respectively. BMS-332 enhances the antigen-specific T cell response. BMS-332 reduces the viral load in the liver and spleen when combined with anti-PD-1 in chronic infection models. BMS-332 can be used for the study of T cell immune checkpoint strategy.

HY-153343A

(S)-Veludacigib	Inhibitor	99.43%
(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-135898

DGK-IN-1	Inhibitor	98.67%
DGK-IN-1 is a DGK inhibitor (DGKa/DGKz IC₅₀: 0.65/0.25 μM). DGK-IN-1 is a T cell activator that can be used in cancer and viral infection research.

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-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-156574

DGKζ-IN-4	Inhibitor	99.52%
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 research.

HY-122949

Momordicine I	Inhibitor
Momordicine I is a cucurbitane-type triterpenoids. Momordicine I suppresses glioma growth by promoting apoptosis and impairing mitochondrial oxidative phosphorylation. Momordicine I inhibits glycolysis, lipid metabolism, induces autophagy in HNC cells to suppress head and neck cancer growth. Momordicine I alleviates isoproterenol-induced cardiomyocyte hypertrophy through suppression of PLA2G6 and DGK-ζ. Momordicine I exerts its cardiovascular benefits by upregulating nitric oxide, inhibiting the activity of angiotensin-converting enzyme (ACE), activating the PI3K/Akt pathway, reducing oxidative stress and inflammation. Momordicine I inhibits AKT1, IL-6, and SRC, suggesting its potential application in type 2 diabetes.

HY-153793

Alcudacigib	Inhibitor
Alcudacigib (ASP1570; DGKζ-IN-1) is an orally active diacylglycerol kinase ζ (DGKζ) inhibitor, with an IC₅₀ of 4.7 nM against human DGKζ and an IC₅₀ of 3.0 nM against mouse DGKζ. Alcudacigib selectively inhibits the kinase activity of DGKζ and induces proteasome-dependent degradation of DGKζ protein. Alcudacigib enhances the anti-tumor functions of T cells and NK cells. Alcudacigib can be used for the research of advanced/metastatic solid tumors.

HY-149666

BMS-496	Inhibitor	99.72%
BMS-496 is adualDGKα/ζlipid kinase inhibitor, with theIC₅₀of 0.09 (DGKα) and 0.006 μM (DGKζ).

HY-171051

Pasodacigib	Inhibitor	98.64%
DGKα-IN-9 (example 298) is an inhibitor of DGKα.

HY-121638

CU-3	Inhibitor
CU-3 is a DGKα inhibitor with an IC₅₀ of 0.6 μM. CU-3 competitively reduces DGKα’s affinity for ATP via binding to the enzyme’s catalytic region. CU-3 induces apoptosis in cancer cells. CU-3 promotes T-cell activation and enhances IL-2 production. CU-3 can be used for the research of hepatocellular carcinoma and cervical cancer.

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DGK

DGK Related Products (45)

Antibodies (2)

DGK Related Products (45):