产品描述
R 59-022 is a 5-HTR antagonist and activates protein kinase C (PKC). R 59-022 is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
体外活性
R 59-022 is able to interrupt thrombin-induced inositol lipid cycling at the level of diacylglycerol and leads to an elevation of protein kinase C activity, in the intact platelet. R 59-022 blocks entry of EBOV pseudotypes in a concentration-dependent manner (IC50: ~5 μM). 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 dose-dependent decreases in entry by the VLPs harboring the EBOV GP (IC50: ~2 μM). 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 Ca2+ by thrombin in either the presence or the absence of extracellular Ca2+. 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[1][2][5].
Cas No.
93076-89-2
分子式
C27H26FN3OS
分子量
459.58
别名
Diacylglycerol kinase inhibitor I;DKGI-I;R 59-022
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years