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.

TRAP1-IN-1 (compound 35) is a selective TRAP1 inhibitor that disrupts TRAP1 tetramer stability, induces degradation of TRAP1 downstream proteins, inhibits OXPHOS, and disrupts mitochondrial membrane potential.

TRAP1-IN-2, also known as compound 36, is a selective degrader of the TRAP1 client protein that does not affect Hsp90-cytosolic clients. It inhibits oxidative phosphorylation (OXPHOS) and shifts cellular metabolism toward glycolysis. Additionally, TRAP1-IN-2 compromises the stability of the TRAP1 tetramer and disrupts the mitochondrial membrane potential [1].

nociceptin/orphanin FQ (NOP) receptor antagonist

TRAP-14 amide is a protease-activated receptor (PAR) activating peptide and acts as a PAR agonist, with an EC50 of 24 μM. It induces significant platelet aggregation via ADP and MMP-2 dependent pathways and is insensitive to Aspirin. Additionally, TRAP-14 amide effectively increases the surface expression of glycoprotein (GP) Ib and GPIIb/IIIa, as well as the release of ADP.

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.

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

Luminespib (VER-52296) is an HSP90 inhibitor that inhibits HSP90α and HSP90β (IC50=7.8/21 nM). Luminespib has antitumor activity and is used in studies of head and neck tumors, among others.

Delmitide, a TNF-alpha production inhibitor, is used potentially for the treatment of Crohn's disease and ulcerative colitis.

NVP-HSP990 (HSP990) is an effective and specific HSP90α/β inhibitor (IC50: 0.6 /0.8 nM).

SW02 is a potent ATPase activator of Hsp70 (EC50: 150 μM). SW02 is able to accumulate total tau and phosphorylated tau (pTau).

SNX2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM.

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 sulfate (Zontivity) is a potent and orally active thrombin receptor (PAR-1) antagonist.

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.

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.

CYPMPO is a free radical spin trap with excellent trapping capabilities toward hydroxyl and superoxide radicals in biological and chemical systems. Decay of the superoxide adduct of CYPMPO proceeds in an apparent first order fashion with half-lives of 15 and 51 minutes in a UV-illuminated hydrogen peroxide solution and a hypoxanthine/xanthine oxidase system, respectively. CYPMPO traps superoxide radicals generated by bovine neutrophils as effectively as DEPMPO.[1] The high melting point (126°C), low hygroscopic properties, and long shelf-life in aqueous solutions offer significant practical advantages for use of CYPMPO over DEPMPO and DMPO.

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 .

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

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

TRAP-6 amide TFA is a thrombin receptor agonist peptide targeting PAR-1.

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.