1. GPCR/G Protein
    Apoptosis
  2. Protease Activated Receptor (PAR)
    Apoptosis
  3. RWJ-56110

RWJ-56110 

目录号: HY-108556
产品使用指南

RWJ-56110 是一种有效的、选择性的、拟肽抑制剂,抑制 PAR-1 激活和内化 (结合 IC50=0.44 uM),对 PAR-2, PAR-3 和 PAR-4 无影响。RWJ-56110 抑制由 SFLLRN-NH2 (IC50=0.16 μM) 和凝血酶 (IC50=0.34 μM) 诱导的血小板聚集,相对于 U46619 (HY-108566) 具有相当的选择性。RWJ-56110 在体内阻断血管生成和新血管的形成。RWJ-56110 诱导细胞凋亡 (apoptosis)。

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RWJ-56110 Chemical Structure

RWJ-56110 Chemical Structure

CAS No. : 252889-88-6

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生物活性

RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 inhibits angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis[1][2].

IC50 & Target

IC50: 0.44 uM (PAR-1)
IC50: 0.16 μM (the aggregation of human platelets induced by SFLLRN-NH2)
IC50: 0.34 μM (the aggregation of human platelets induced by thrombin)[1][2]

体外研究
(In Vitro)

Proteinase-activated receptors (PARs) are a family of G protein-coupled receptors activated by the proteolytic cleavage of their N-terminal extracellular domain, exposing a new amino terminal sequence that functions as a tethered ligand to activate the receptors.
RWJ56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM) while being quite selective relative to collagen and the thromboxane mimetic U46619 (HY-108566)[1].
RWJ-56110 is fully inhibits thrombin-induced RASMC proliferation with an IC50 value of 3.5 μM. RWJ-56110 shows blockade of thrombin’s action with RASMC calcium mobilization (IC50=0.12 μM), as well as with HMVEC (IC50=0.13 μM) and HASMC calcium mobilization (IC50=0.17 μM)[1].
RWJ56110 (0.1-10 μM; 24-96 hours) inhibits endothelial cell growth dose-dependently, with half-maximal inhibitory concentration of RWJ56110 is approximately 10 μM[2].
RWJ56110 (0.1-10 μM; 6 hours) inhibits DNA synthesis of endothelial cells in a thymidine incorporation assays. Endothelial cells are in fast-growing state (50-60% confluence), RWJ56110 inhibits cell DNA synthesis in a dose-dependent manner, but when cells that are in the quiescent state (100% confluent), the inhibitory effect of PAR-1 antagonists is much less pronounced[2].
RWJ56110 (0.1-10 μM; pretreatment for 15 min) inhibits thrombin-induced Erk1/2 activation in a concentration-dependent manner. However, when endothelial cells are stimulated by FBS (final concentration 4%), it reduces partially the activated levels of Erk1/2[2].
RWJ56110 (30 μM; 24 hours) has an inhibitory effect on endothelial cell cycle progression. It reduces the percentage of cells in the S phase, while alterations in the percentages of G1 and G2/M cells are less pronounced[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: Endothelial cells
Concentration: 0 μM; 3 μM; 1 μM; 3 μM; 10 μM
Incubation Time: Pretreatment for 15 min
Result: Resulted in MAPK activation in Endothelial cells.

Cell Cycle Analysis[2]

Cell Line: Endothelial cells
Concentration: 0 μM; 3 μM; 1 μM; 3 μM; 10 μM
Incubation Time: Pretreatment for 15 min
Result: Reduced cell number in S phase.
分子量

790.73

Formula

C41H43Cl2F2N7O3

CAS 号
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.

参考文献
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RWJ-56110
目录号:
HY-108556
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