二酰甘油激酶抑制剂II

二酰甘油激酶抑制剂II用途

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

二酰甘油激酶抑制剂II名称

[ CAS 号 ]:
120166-69-0

[ 中文名 ]:
二乙酰基甘油激酶抑制剂II

[ 英文名 ]:
R59949

[英文别名 ]:

MFCD00069258
Diacylglycerol Kinase Inhibitor II

二酰甘油激酶抑制剂II生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 表观遗传学 >> PKC

研究领域 >> 癌症

信号通路 >> TGF-beta/Smad 信号通路 >> PKC

[体外研究]

在R59949存在的情况下,加压素和胶原诱导的释放反应和聚集强烈增加,与花生四烯酸代谢物的形成无关[1]。在THP-1单核细胞中,R59949以8.6μM的半最大浓度减弱CCL2诱发的Ca2+信号[2]。R59949通过减少血管平滑肌细胞跨质膜L-精氨酸的摄取来抑制诱导型一氧化氮的产生[4]。

[参考文献]

[1]. de Chaffoy de Courcelles D, et al. The role of endogenously formed diacylglycerol in the propagation and termination of platelet activation. A biochemical and functional analysis using the novel diacylglycerol kinase inhibitor, R 59 949. J Biol Chem. 1989;264(6):3274-3285.

[2]. Day P, et al. Inhibitors of DAG metabolism suppress CCR2 signalling in human monocytes. Br J Pharmacol. 2019;176(15):2736-2749.

[3]. Meinhardt G, et al. Effect of novel modulators of protein kinase C activity upon chemotherapy-induced differentiation and apoptosis in myeloid leukemic cells. Anticancer Drugs. 2002;13(7):725-733.

[4]. Shimomura T, et al. R59949, a diacylglycerol kinase inhibitor, inhibits inducible nitric oxide production through decreasing transplasmalemmal L-arginine uptake in vascular smooth muscle cells. Naunyn Schmiedebergs Arch Pharmacol. 2017;390(2):207-214.

二酰甘油激酶抑制剂II物理化学性质

[ 密度 ]:
1.36g/cm3

[ 沸点 ]:
637.1ºC at 760mmHg

[ 分子式 ]:
C₂₈H₂₅F₂N₃OS

[ 分子量 ]:
489.57900

[ 闪点 ]:
339.1ºC

[ 精确质量 ]:
489.16900

[ PSA ]:
73.12000

[ LogP ]:
5.87310

[ 蒸汽压 ]:
3.94E-16mmHg at 25°C

[ 折射率 ]:
1.688

[ 储存条件 ]:
-20°C

二酰甘油激酶抑制剂II安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

[ 危险品运输编码 ]:
NONH for all modes of transport

二酰甘油激酶抑制剂II文献

Diacylglycerol kinase α promotes 3D cancer cell growth and limits drug sensitivity through functional interaction with Src.

Oncotarget 5(20) , 9710-26, (2014)

Diacylglycerol kinase (DGK)α converts diacylglycerol to phosphatidic acid. This lipid kinase sustains survival, migration and invasion of tumor cells, with no effect over untransformed cells, suggesti...

Insulin action on polyunsaturated phosphatidic acid formation in rat brain: an "in vitro" model with synaptic endings from cerebral cortex and hippocampus.

Neurochem. Res. 34(7) , 1236-48, (2009)

The highly efficient formation of phosphatidic acid from exogenous 1-stearoyl-2-arachidonoyl-sn-glycerol (SAG) in rat brain synaptic nerve endings (synaptosomes) from cerebral cortex and hippocampus i...

Effect of novel modulators of protein kinase C activity upon chemotherapy-induced differentiation and apoptosis in myeloid leukemic cells.

Anticancer Drugs 13(7) , 725-33, (2002)

Modulation of protein kinase C (PKC) activity has been demonstrated to either prevent or enhance drug-induced apoptosis in various tissue types. We tested four novel modulators of PKC activity in comp...

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