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R 59-022 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
R 59-022 hydrochloride图片
CAS NO:93076-98-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
DKGI-I hydrochloride
Diacylglycerol kinase inhibitor I hydrochloride
产品介绍
R 59-022 (DKGI-I) hydrochloride 是一种DGK抑制剂 (IC50: 2.8 μM)。R 59-022 抑制 OAG 磷酸化为 OAPA。R 59-022 hydrochloride 是一种5-HT Receptor拮抗剂,可激活蛋白激酶 C (PKC)。R 59-022 增强血小板中凝血酶诱导的甘油二酯的产生,并抑制嗜中性粒细胞中磷脂酸的产生。
生物活性

R 59-022 (DKGI-I) hydrochloride is aDGKinhibitor (IC50: 2.8 μM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a5-HT Receptorantagonist, and activatesprotein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils[1][2][3][4].

IC50& Target[4]

PKC

 

serotonin

 

DGK

2.8 μM (IC50)

体外研究
(In Vitro)

R 59-022 (10 μM,1 分钟) hydrochloride 增强聚集,但不会增强由次最大浓度的凝血酶引起的形状变化[2]
R 59-022 (30 μM,0-60 分钟) hydrochloride 增加嗜铬细胞中去甲肾上腺素的释放[3]
R 59-022 (40 μM,30 分钟) hydrochloride 激活 HeLa 和 U87 细胞中的 PKC[4]
R 59-022 (0-10 μM,4 小时) hydrochloride 阻断 EBOV GP 介导的进入 Vero 细胞[5]

Western Blot Analysis[4]

Cell Line:HeLa cells
Concentration:40 uM
Incubation Time:30 min
Result:Increased the phosphorylation of PKC downstream targets by about 2.5-fold.
体内研究
(In Vivo)

R 59-022 (2 mg/kg,腹腔注射,12 天) hydrochloride 显着增加植入 U87 GBM 细胞的 SCID 小鼠的中位生存期[6]

Animal Model:SCID mice implanted with U87 GBM cells[6]
Dosage:10 mg/kg
Administration:Intraperitoneal injection (i.p.)
Result:Increased median survival and decreased tumor volume.
分子量

496.04

Formula

C27H27ClFN3OS

CAS 号

93076-98-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.