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93076-89-2

中文名稱 化合物 T16709
英文名稱 DIACYLGLYCEROL KINASE INHIBITOR I
CAS 93076-89-2
分子式 C27H26FN3OS
分子量 459.58
MOL 文件 93076-89-2.mol
更新日期 2023/03/20 15:41:21
93076-89-2 結(jié)構(gòu)式 93076-89-2 結(jié)構(gòu)式

基本信息

中文別名
甘油二酯激酶
二乙酰基甘油激酶
化合物 T16709
二?;视图っ?/DGK-Ε抗體
英文別名
DKI
DAGK
DGKE
DGKI
DAGK4
DAGK7
DGK-θ
R59022
DKGI-I
DAG KINASE

物理化學(xué)性質(zhì)

儲存條件-20°C
溶解度0.1 M HCl: slightly soluble
形態(tài)solid
顏色pale yellow
穩(wěn)定性可在-20°C下的DMSO中的溶液儲存長達(dá)3個(gè)月。

安全數(shù)據(jù)

安全說明23-24/25
WGK Germany3

常見問題列表

生物活性
R 59-022 (DKGI-I) 是一種二酰甘油激酶 (diacylglycerol kinase) 抑制劑 (IC50=2.8 μM)。R 59-022 是一種 5-HTR 拮抗劑,激活蛋白激酶 C (PKC)。R 59-022 增強(qiáng)凝血酶誘導(dǎo)血小板產(chǎn)生二酰甘油和抑制中性粒細(xì)胞產(chǎn)生磷脂酸。
靶點(diǎn)

PKC

serotonin

diacylglycerol kinase

2.8 μM (IC 50 )

體外研究

In the intact platelet, R 59-022 is able to interrupts thrombin-induced inositol lipid cycling at the level of diacylglycerol and leads to an elevation of protein kinase C activity.
R 59-022 (10 μM) potentiates aggregation, but not shape change induced by sub-maximal concentrations of thrombin. R59022 (10 μM) had no significant effect on the dose-response curve for the mobilization of intracellular Ca 2+ by thrombin in either the presence or the absence of extracellular Ca 2+ .
R 59-022, an inhibitor of filovirus entry, prevents the macropinocytic uptake of filoviral particles, inhibits entry mediated by multiple filovirus GPs, and blocks replicative EBOV growth. R 59-022 blocks entry of EBOV pseudotypes in a concentration-dependent manner (IC 50 : ~5 μM). R 59-022 dose-dependent decreases in entry by the VLPs harboring the EBOV GP (IC 50 : ~2 μM). R 59-022 (2-12 μM; 1 hour) can inhibit EBOV GP-mediated entry in multiple cell types. R 59-022 (5 μM; 30 minutes) blocks macropinocytosis in vero cells.

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