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R 59-022

CAS No. : 93076-89-2

MCE 站：R 59-022

产品活性：R 59-022 (DKGI-I) 是一种二酰甘油激酶 (diacylglycerol kinase) 抑制剂 (IC₅₀=2.8 μM)。R 59-022 是一种 5-HTR 拮抗剂，激活蛋白激酶 C (PKC)。R 59-022 增强凝血酶诱导血小板产生二酰甘油和抑制中性粒细胞产生磷脂酸。

研究领域：Epigenetics  |  TGF-beta/Smad  |  GPCR/G Protein  |  Neuronal Signaling

作用靶点：PKC  |  5-HT Receptor

In Vitro: 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 Ca²⁺ by thrombin in either the presence or the absence of extracellular Ca²⁺.
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 (IC₅₀: ~5 ?M). R 59-022 dose-dependent decreases in entry by the VLPs harboring the EBOV GP (IC₅₀: ~2 ?M). R 59-022 (2-12 μM; 1 hour) can inhibit EBOV GP-mediated entry in multiple cell types. R 59-022 (5 ?M; 30 minutes) blocks macropinocytosis in vero cells.

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