2. Signaling Pathways
  3. GPCR/G Protein
  4. Protease Activated Receptor (PAR)
  5. Protease Activated Receptor (PAR) Inhibitor

Protease Activated Receptor (PAR) Inhibitor

Protease Activated Receptor (PAR) Isoform Comparison

Protease Activated Receptor (PAR) Inhibitors (18):

Cat. No. Product Name Effect Purity
  • HY-P991988
    Anti-PAR1 Antibody
    		Inhibitor
    Anti-PAR1 Antibody is an anti-PAR1 antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).
  • HY-P1260
    FSLLRY-NH2
    		Inhibitor 99.89%
    FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.
  • HY-13965
    Parmodulin 2
    		Inhibitor 99.82%
    Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.
  • HY-120261
    GB-88
    		Inhibitor 98.66%
    GB-88 is an oral, selective non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 μM.
  • HY-148016
    I-287
    		Inhibitor 99.36%
    I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research.
  • HY-108556A
    RWJ-56110 dihydrochloride
    		Inhibitor 99.87%
    RWJ-56110 dihydrochloride 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 dihydrochloride 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 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.
  • HY-P1260A
    FSLLRY-NH2 TFA
    		Inhibitor 98.97%
    FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.
  • HY-124663
    CBK289001
    		Inhibitor 99.74%
    CBK289001 is a tartrate-resistant acid phosphatase (TRAP/ACP5) inhibitor. CBK289001 inhibits TRAP 5bMV, TRAP 5bOX and TRAP 5aOX with IC50s of 125 µM, 4.21 µM and 14.2 µM, respectively.
  • HY-P2933
    Activated protein C
    		Inhibitor
    Activated protein C is an anticoagulant targeting coagulation factors Va and VIIIa. Activated protein C demonstrates cytoprotective effects through binding to endothelial cell protein C receptor (EPCR) and protease-activated receptor-1 (PAR-1), regulating gene expression, anti-inflammation, anti-apoptosis, and stabilizing endothelial barriers. Activated protein C is promising for research of diseases such as severe sepsis and ischemic stroke.
  • HY-105999B
    APC 366 TFA
    		Inhibitor ≥99.0%
    APC 366 (TFA) is an irreversible mast cell tryptase inhibitor. APC 366 (TFA) can be used for the research of allergic diseases.
  • HY-162409
    PAR4 antagonist 4
    		Inhibitor
    PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 42.5 min.
  • HY-181999
    PC8
    		Inhibitor
    PC8 is a selective dual inhibitor of PARP1/CDK6, with an IC50 of 0.126 μM for PARP1 and 0.197 μM for CDK6. PC8 does not alter PARP1 expression, but reduces the expression of its downstream target PAR. PC8 inhibits the canonical Wnt/β-catenin signaling pathway. PC8 induces intracellular ROS accumulation and exacerbates DNA damage. PC8 inhibits the proliferation of triple-negative breast cancer (TNBC) cells. PC8 can be used for the research of triple-negative breast cancer.
  • HY-162408
    PAR4 antagonist 3
    		Inhibitor
    PAR4 antagonist 3 (Compound 36) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 26.1 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 97.6 min.
  • HY-108556
    RWJ-56110
    		Inhibitor
    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.
  • HY-128009
    ML161 analog 1
    		Inhibitor 99.62%
    ML161 analog 1 (compound 38) is an analog of ML161 (HY-13965). ML161 analog 1 is a selective allosteric inhibitor of PAR1 with an IC50 of 1.68 μM.
  • HY-146333
    TRAP-6-IN-1
    		Inhibitor
    TRAP-6-IN-1 (Compound 8) is a dual collagen and TRAP-6 inhibitor with IC50 values of 17.12 µM and 11.88 µM against collagen and TRAP-6, respectively. TRAP-6-IN-1 inhibits agonist-induced platelet aggregation in a non-competitive manner.
  • HY-169817
    PAR-2-IN-2
    		Inhibitor
    PAR-2-IN-2 (compound P-596) is a protease-activated receptor 2 (PAR-2) inhibitor with an IC50 of 10.79 μM for SLIGKV and an IC50 of greater than 200 μM for Trypsin.
  • HY-108556AR
    RWJ-56110 dihydrochloride (Standard)
    		Inhibitor
    RWJ-56110 dihydrochloride (Standard) is the analytical standard of RWJ-56110 (dihydrochloride) (HY-108556A). This product is intended for research and analytical applications. RWJ-56110 dihydrochloride 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 dihydrochloride 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 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.