R 59-022 hydrochloride

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CAS NO:

93076-98-3

DKGI-I hydrochloride
Diacylglycerol kinase inhibitor I hydrochloride

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.