pbr

PBR28, a TSPO modulator, holds potential for preventative research in Pulmonary Arterial Hypertension (PAH) and is instrumental in brain positron emission tomography (PET) imaging studies through its capacity for radioactive labeling to trace the 18 KDa transporter (TSPO) [1].

PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. This compound is utilized in cancer research.

PBRM1-BD2-IN-3 (compound 12) is a potent inhibitor of PBRM1-BD2, exhibiting an IC50 value of 1.1 μM, and is utilized in anticancer research.

PBRM1-BD2-IN-7, a selective and cell-active inhibitor targeting the polybromo-1 (PBRM1) bromodomain, demonstrates inhibitory efficacy against PBRM1-BD2 with an IC50 value of 0.29 μM. This compound is utilized in cancer research.

PBRM1-BD2-IN-5 is a potent inhibitor of the PBRM1 Bromodomain, demonstrating dissociation constant (Kd) values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and boasts an inhibitory concentration 50 (IC50) value of 0.26 μM for PBRM1-BD2. This compound effectively diminishes the interaction between the full-length PBRM1 and acetylated histone peptide within the PBAF complex in cell lysates, which positions it as a promising candidate for anticancer research.

PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor (PBRM1-BD2 Kd=4.4 μM, PBRM1-BD2 IC50=0.16 μM; PBRM1-BD5 Kd=25 μM). PBRM1-BD2-IN-8 shows anti-cancer activity.

PBRM1-BD2-IN-1 is a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, displaying binding affinity and inhibitory efficacy with Kd and IC50 values of 0.7 μM and 0.2 μM, respectively. This compound is utilized in cancer research.

ß-pBrPh-Glc (ßpBrPhGlc) is an inhibitor of ice recrystallization, controlling the growth of extracellular ice and inhibiting the recrystallization of intracellular ice. ß-pBrPh-Glc may be used as a cryopreservative , possibly with antioxidant activity.

PBRM1-BD2-IN-6, a potent inhibitor of the PBRM1 bromodomain, exhibits an IC50 value of 0.22 µM and demonstrates antiproliferative activity. It holds potential for research in PBRM1-dependent cancer treatment.

PBRM is the first selective, potent, non-estrogenic, irreversible inhibitor of 17β-HSD1.

DAA-1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), acting as a potent and selective agonist at the peripheral benzodiazepine receptor.

high affinity agonist of the translocator protein

Orphenadrine hydrochloride (Mephenamin) is a muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.

Orphenadrine Citrate (Flexon) is a skeletal muscle relaxant, it acts in the central nervous system to produce its muscle relaxant effects.