diacylglycerol kinase a

R59949 是一种泛二酰甘油激酶(DGK)抑制剂，IC50为 300 nM。它通过提高内源性配体二酰甘油水平来激活蛋白激酶 C(PKC)。它强烈抑制 Ⅰ 型 DGKα 和 γ 的活性，中度减弱 Ⅱ 型 DGKθ 和 κ 的活性。

R 59-022 (DKGI-I) 是一种二酰基甘油激酶 （DGK） 抑制剂，也 是一种 5-HT Receptor 拮抗剂，可阻断宿主细胞中的丝状病毒内化。R 59-022 可激活蛋白激酶 C (PKC)，抑制肠平滑肌的收缩力，增强由1-油酰基-2-乙酰甘油诱导的 O2-产生。

Dioctanoylglycol (ethane-1,2-diyl dioctanoate) 是二酰基甘油类似物，也是二酰基甘油激酶 (DGK) 抑制剂，其Ki=为58 μM。

CU-3 is a potent and selective inhibitor of diacylglycerol kinase alpha (DGKalpha). CU-3 attenuates cancer cell proliferation and simultaneously enhances immune responses including anti-cancer immunity.

Protein kinase C (PKC ) is a calcium-independent, phospholipid- and diacylglycerol-dependent serine threonine kinase involved in diverse signaling pathways, including those involved in neuronal signaling, cytoskeletal function, and inflammation.[1] PKC inhibitor peptide is a synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKC .[2] It selectively and reversibly inhibits the translocation of PKC to intracellular membranes, blocking activation.[2] PKC inhibitor peptide is commonly used in cells to evaluate the role of PKC in various cellular responses.[3],[4],[5]

C8 D-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It is cytotoxic to U937 cells (IC50 = 17 μM) and induces nuclear DNA fragmentation 5- to 6-fold more potently than C8 ceramide . C8 D-threo Ceramide is a substrate for E. coli diacylglycerol kinase. It activates ceramide-activated protein kinase (CAPK) in U937 cells. C8 D-threo Ceramide also enhances V. cholerae cytolysin pore formation in liposome lipid membranes, as measured by calcein release, with a 50% release dose (RD50) value of ~5 μg ml.

1,2-Dioleoyl-rac-glycerol-13C3 is intended for use as an internal standard for the quantification of 1,2-dioleoyl-rac-glycerol by GC- or LC-MS. 1,2-dioleoyl-rac-glycerol is a diacylglycerol that contains oleic acid at the sn-1 and sn-2 positions. It effectively binds the C1 domain to activate conventional protein kinase C forms and serves as a substrate for diacylglycerol kinases and multisubstrate lipid kinase.1,2,3 |1. Yamaguchi, Y., Shirai, Y., Matsubara, T., et al. Phosphorylation and up-regulation of diacylglycerol kinase γ via its interaction with protein kinase Cγ. J. Biol. Chem. 281(42), 31627-31637 (2006).|2. Zhou, Q.Z., Raynor, R.L., Wood, M.G., Jr., et al. Structure-activity relationship of synthetic branched-chain distearoylglycerol (distearin) as protein kinase C activators. Biochemistry 27(19), 7361-7365 (1988).|3. Epand, R.M., Shulga, Y.V., Timmons, H.C., et al. Substrate chirality and specificity of diacylglycerol kinases and the multisubstrate lipid kinase. Biochemistry 46(49), 14225-14231 (2007).

Phosphatidic acid is a phospholipid and an intermediate in glycerolipid biosynthesis. It is a transient intermediate in the synthesis of various phospholipid species that is synthesized de novo in cells via multiple routes, including the glycerol-3 phosphate and dihydroxyacetone phosphate pathways, enzymatic conversion of phosphatidylcholine by phospholipase D, and acetylation of lysophosphatidic acid by lysoPA-acyltransferase, among others. It has roles in shaping cellular membranes, cellular signaling, vesicle fission and fusion, as well as mitochondrial division and fusion. It stimulates respiratory burst in neutrophils independent of diacylglycerol and activates monoacylglycerol acyltransferase, phospholipase C (PLC), Ras, and phosphatidylinositol 4-phosphate (PIP4) kinase in several cell lines. Phosphatidic acids (egg) is a mixture of phosphatidic acids isolated from chicken egg with fatty acids of variable chain lengths.

JNJ-3790339 是Ritanserin 的类似物，是选择性的、有效的二酰甘油激酶 (DGKα) 抑制剂(IC50: 9.6 μM)，能够上调 T 细胞的活化，并对恶性细胞有诱导毒性作用。

Cochlioquinone A is an inhibitor of diacylglycerol kinase (DGK) and diacylglycerol acyltransferase (DGAT). It has been shown to reduce the concentration of phosphatidic acid in T cell lymphoma and has also been shown to compete with macrophage inflammatory protein-1α for binding to human CCR5 chemokine receptors.

QNN33358 is an alkylacylglycerol acts as a protein kinase C (PKC) inhibitor and diacylglycerol (DAG) antagonist.

BAY 2965501 是一种有效且具有的选择性二酰基甘油激酶 zeta (DGKζ) 抑制剂，诱导 pERK 激活。BAY 2965501 可用于研究癌症。

BMS-502 是一种二酰基甘油激酶 (DGK) α 和 ζ 的强效双重抑制剂， 诱导人和小鼠T细胞的免疫反应，阻断 T 细胞中细胞内检查点信号传导。BMS-502 以剂量依赖的方式刺激免疫反应，可用于研究与免疫相关的疾病。

AMB639752为一种高效DGKα抑制剂，能通过抑止整合体内DGKα活性，复原因重复刺激导致的SAP缺失型淋巴细胞的细胞死亡(RICD)。此化合物适合于X连锁淋巴增生性疾病1(XLP-1)的相关研究。

DGKα-IN-6，一种DGKα抑制剂，其IC50值为1.377 nM，显示出可能用于癌症研究。

DGKα-IN-8（Example 51）是DGKα的高效抑制剂，其IC50值为22.491 nM，EC50值为0.256 nM。该化合物主要用于癌症（含实体瘤）及HIV和乙型肝炎病毒感染的研究领域。

JH-131e-153, 作为一种二酰基甘油(DAG)内酯，具有激活 Munc13-1 的功能，靶向其 C1 结构域。JH-131e-153 对 Munc13-1 激活效率表现为 WT>I590≈R592A≈W588A。值得注意的是，Munc13-1 的 C1 结构域与蛋白激酶 C (PKC) 在序列和结构上具有同源性。对于 Munc13-1 和 PKC 的激活效率，JH-131e-153 的效果排序为 PKCα>Munc13-1>PKCε。该化合物通过调节 Munc13-1，对神经元过程产生影响，因此可用于神经退行性疾病的相关研究。

Protein kinase D (PKD), a serine threonine protein kinase activated by diacylglycerol downstream of PKC signaling, has three human isoforms that modulate cell proliferation, survival, invasion, and protein transport. CRT0066101 acts as an inhibitor of these three PKD isoforms, with IC50 values of 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively. It demonstrates selectivity for PKD over a range of more than 90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. This specificity allows CRT0066101 to inhibit cell proliferation, induce apoptosis, and notably reduce the viability of pancreatic cancer cells both in vitro and in vivo.

Diacylglycerols (DAG) are generated through the hydrolysis of membrane phospholipids and function as lipid second messengers by activating protein kinase C (PKC) and modulating cell growth and apoptosis. Additionally, they act as precursors for DAG kinases in the synthesis of phosphatidic acid, a crucial lipid messenger. The compound 1-NBD-decanoyl-2-decanoyl-sn-glycerol incorporates a nitrobenzoxadiazole (NBD) fluorophore at the ω-end of its terminal decanoyl chain, using the structure of 1,2-didecanoyl-sn-glycerol as a model for diacylglycerol. This molecule is expected to exhibit excitation and emission peaks at roughly 470/541 nm, paralleling those of various NBD-labeled phospholipids. Fluorescently labeled lipids, such as this, are instrumental in exploring their interactions with proteins, their uptake by cells and liposomes, and in developing assays for lipid metabolism research.

ZKN14489, also known as 08:0 DG and 1,2-dioctanoyl-sn-glycerol, is a short-chain, cell-permeable diacylglycerol that serves as a lipid cofactor for activating protein kinase C.

1,3-Dioleoyl glycerol, a diacylglycerol with oleic acid at the sn-1 and sn-3 positions, activates protein kinase C (PKC) by approximately 30% at a concentration of 50 μM.

1-Palmitoyl-d9-2-palmitoyl-sn-glycerol serves as an internal standard for quantifying 1,2-dipalmitoyl-sn-glycerol using GC or LC-MS techniques. This diacylglycerol, featuring palmitic acid at both the sn-1 and sn-2 positions, stimulates protein kinase C (PKC) activity by 15% at a 25 μM concentration. Additionally, 1,2-dipalmitoyl-sn-glycerol encourages rapid growth in Frankia, a genus of Gram-positive bacteria.