trap-1

TRAP-1 (XJZ-06-462) is a p53 transcription activator that effectively activates mutant p53 and triggers the transcription of p53 target genes. In the p53Y220C pancreatic cell line, TRAP-1 rapidly upregulates p21 and other p53 target genes. TRAP-1 also inhibits cell proliferation, exhibiting IC50 values of 3.94 μM and 0.531 μM in BxPC-3 and A549 cell lines, respectively. Additionally, TRAP-1 modulates autophagy in lung cancer cells and provides protection against oxidative stress and apoptosis.

TRAP-6-IN-1 (Compound 8) is a dual inhibitor of collagen and TRAP-6 with IC50 values of 17.12 μM and 11.88 μM, respectively. It non-competitively inhibits agonist-induced platelet aggregation[1].

nociceptin orphanin FQ (NOP) receptor antagonist

DP-1 hydrochloride is a degradation product of SDC-TRAP-0063, a fragment of Ganetespib, a heat shock protein 90 (HSP90) inhibitor with antitumor activity.

DMPO (5,5-Dimethyl-1-pyrroline N-oxide) is a kind of water-soluble nitric oxide spin trap, which allows the measurement of oxygen-centered free radicals in biological systems at room temperature using electron spin resonance. It has a high reaction rate constant for superoxide and hydroxyl radicals and distinguishes simultaneously among a variety of important biologically generated free radicals.

Vorapaxar (MK-5348) (SCH 530348) is an effective and orally active thrombin receptor (PAR-1) antagonist (Ki: 8.1 nM).

NFAT Inhibitor (VIVIT peptide) is a cell-permeable compound that selectively inhibits the calcineurin-mediated dephosphorylation of NFAT.

PU-H54 is a purine-based inhibitor of Grp94. It is a Grp94-selective resorcinol-based inhibitor isolated through probing of the exclusive binding region of S2 subpocket in Grp94.

TRAP-6 amide acetate is a PAR-1 thrombin receptor agonist peptide[1].

Thrombin receptor agonist peptide (TRAP-14) is a 14-amino acid peptide agonist of the α-thrombin receptor. It induces aggregation of washed platelets as well as platelets in citrated and hirudin plasma. TRAP-14 (100 μM) increases the cytosolic calcium concentration in isolated guinea pig pulmonary smooth muscle cells 5-fold over baseline. It increases pulmonary arterial pressure in isolated guinea pig lung when used at a concentration of 1 μM, which is comparable to the effect induced by 10 nM α-thrombin. TRAP-14 also induces contraction of isolated rat aortic rings and increases endothelin-1 (ET-1) levels in a dose-dependent manner, an effect that is reversed by the ETA antagonist BQ-123 and the nitric oxide synthase (NOS) inhibitor L-NNA .

Hepcidin-1 (mouse) is a peptide hormone that regulates iron balance, elevates mRNA for TRAP, cathepsin K, and MMP-9, and promotes TRAP-5b protein secretion. This compound also reduces FPN1 protein levels and boosts intracellular iron, ultimately aiding in osteoclast differentiation [1].

TRAP-6 (Thrombin Receptor Activator Peptide 6)(2TFA) is an agonist of protease-activated receptor 1 (PAR1).

TRAP-6 amide, a PAR-1 thrombin receptor agonist peptide, [Cyclo(Pro-Arg-Gly)-Arg-Ser-Gly], is derived from the primary sequence of [TRAP-2].

Thrombin Receptor Activator for Peptide 5 (TRAP-5), also known as Coagulation Factor II Receptor (1-5) or Proteinase Activated Receptor 1 (1-5), is utilized in coronary heart disease (CHD) research.

9(Z)-Pentacosene is a cuticular hydrocarbon and insect sex hormone.1,2,3 It is found in the cuticle of female F. canicularis flies and is an attractant to males in a trap assay.1 9(Z)-Pentacosene is a contact sex hormone in scarab beetles and locust borers that is more abundant in females than males.2,3 It elicits arrestment, alignment, and mounting by males of both species in mating assays but only elicits copulation by the locust borer. 9(Z)-Pentacosene is also produced by the orchid O. exaltata and by C. cunicularius, a pollinator of O. exaltata.4

TRAP-6 peptide is a hexapeptide corresponding to residues 42-47 of protease-activated receptor 1 (PAR1). It acts as an agonist of PAR1, inducing platelet aggregation in human platelet-rich plasma ex vivo (EC50 = 0.8 μM). TRAP-6 (0.3 and 0.6 mg/kg) has a triphasic effect on mean arterial blood pressure (MAP) in anesthetized rats with a short decrease, an increase, and then a longer decrease in MAP following intravenous administration.

Hepcidin-1 (mouse) TFA, an endogenous peptide hormone, regulates iron homeostasis by upregulating mRNA levels of TRAP, cathepsin K, and MMP-9, enhancing TRAP-5b protein secretion, and downregulating FPN1 protein levels, thereby increasing intracellular iron. It also promotes osteoclast differentiation [1].

VER-82576 (NVP-BEP800), a synthetic HSP90β inhibitor (IC50: 58 nM), exhibits >70-fold selectivity against Hsp90 family members Trap-1 and Grp94.

DP-1, a Ganetespib degradation product, represents a fragment derived from SDC-TRAP-0063. Ganetespib itself functions as an inhibitor of heat shock protein 90 (HSP90), exhibiting notable anti-tumor properties.

TRAP-7, a thrombin receptor (PAR) activating peptide, stimulates total inositol phosphate (IP) accumulation and phosphorylation of a specific endogenous substrate for activated PKC. TRAP-7 can be utilized in cardiovascular disease research [1].

2-chloro Palmitic acid is a monochlorinated form of palmitic acid . It is produced in a myeloperoxidase (MPO) and time-dependent manner in neutrophils stimulated by phorbol 12-myristate 13-acetate . 2-chloro Palmitic acid (10 μM) induces neutrophil extracellular trap (NET) formation (NETosis) in human neutrophils, increasing DNA release from neutrophils, colocalization of MPO with extracellular DNA (ecDNA), and trapping of E. coli. It increases COX-2 protein levels in human coronary artery endothelial cells (HCAECs) when used at a concentration of 50 μM and increases production of P-selectin, von Willebrand factor, and angiopoietin-2 in HCAECs, as well as neutrophil and platelet adherence, when used at a concentration of 10 μM. 2-chloro Palmitic acid (10-50 μM) also induces apoptosis in THP-1 cells and primary human monocytes and increases caspase-3 activity in THP-1 cells.

SH491 (Compound 33) serves as an antiosteoporosis agent, effectively inhibiting RANKL-induced osteoclast differentiation in bone-marrow-derived monocytes (BMMs) with an IC50 of 11.8 nM. Additionally, SH491 suppresses the expression of genes and proteins related to osteoclastogenesis, specifically TRAP, CTSK, MMP-9, and ATPase v0d2 [1].

iso-TRAP-6 (iso-SFLLRN), a hexapeptide derived from the substitution of isoserine for serine, is a protease-activated receptor 1 (PAR1) agonist that activates platelets via PAR-1. iso-TRAP-6 is more resistant to degradation by plasma aminopeptidases than iso-TRAP-6.

Inclacumab (Anti-Human selectin P Recombinant Antibody) is a fully humanized IgG4 monoclonal antibody that selectively binds to P-selectin. Inclacumab inhibits platelet leukocyte aggregation induced by thrombin receptor-activating peptide (TRAP) or adenosine diphosphate (ADP). Inclacumab inhibits platelet leukocyte aggregation induced by thrombin receptor activating peptide (TRAP) or adenosine diphosphate (ADP).