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

RWJ-56110 

Cat. No.: HY-108556
Handling Instructions

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 blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis.

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RWJ-56110 Chemical Structure

RWJ-56110 Chemical Structure

CAS No. : 252889-88-6

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Description

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 blocks 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]

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].

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.
Molecular Weight

790.73

Formula

C₄₁H₄₃Cl₂F₂N₇O₃

CAS No.

252889-88-6

SMILES

O=C(N[[email protected]](C(NCC1=CC=CC=C1)=O)CCN)[[email protected]@H](NC(NC2=CC3=C(C=C2)C(CN4CCCC4)=CN3CC5=C(Cl)C=CC=C5Cl)=O)CC6=CC=C(F)C(F)=C6

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

RWJ-56110RWJ56110RWJ 56110Protease-Activated Receptor (PAR)ApoptosisThrombin receptorsAngiogenesisDNA synthesisendothelial cellsRASMCHMVECmimeticInhibitorinhibitorinhibit

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RWJ-56110
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