pbr

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

high affinity agonist of the translocator protein

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].

FG8119 is a novel benzodiazepine agonist with potential anticonvulsant and antiepileptic activity for studying neurological disorders.

CGS8216 is a benzodiazepine receptor antagonist that shows analgesic activity at high doses.CGS8216 has anxiolytic activity and may be used to study immune system disorders.

CGS 20625 is an orally active, specific, and potent partial agonist at the central benzodiazepine receptor with anxiolytic and anticonvulsant activity.CGS 20625 inhibits the binding of [3H]-flunitrazepam to the central benzodiazepine receptor and can be used in studies of neurological disorders such as anxiety and epilepsy.

Emapunil (XBD-173) is an anxiolytic drug which acts as a selective agonist at the peripheral benzodiazepine receptor, also known as the mitochondrial 18 kDa translocator protein or TSPO.

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.

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

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

PBRM1-BD2-IN-3 (compound 12) is a potent PBRM1-BD2 inhibitor with an IC50 of 1.1 μM, used in anticancer research.

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

PBRM (17β-HSD1-IN-2) is a selective covalent inhibitor of 17β-HSD1, used in breast cancer and endometriosis research.

PBRM1/SMARCA2,4 binder-1 is an agent that binds to PBRM1, SMARCA2, and SMARCA4, with IC50 values of 0.083 μM, 0.153 μM, and 0.046 μM, respectively.

PBRM1/SMARCA2,4-ligand-1 (Compound 4) serves as a ligand for the target protein PROTAC, capable of binding to PBRM1, SMARCA2, and SMARCA4. It is a potent inhibitor of the SMARCA4 bromodomain and is utilized in the synthesis of PROTAC AU-24118.

5-MeO-NBpBrT (Compound 2f) (5MT-NB4B) is an NBOMe derivative and an N-(bromobenzyl) isomer based on 5MT.

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-1 is a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibiting a binding affinity (Kd) of 0.7 μM and an inhibitory efficacy (IC50) of 0.2 μM, and is used in cancer research.

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.

BrBzGCp2 (p BrBzGSH(Cp)2) is an inhibitor of glyoxalase 1 (GLO1) with antitumor and neuroprotective activity. It can alleviate anxiety and be used in neurodegenerative disease research.

MS417 (GTPL7512) is an inhibitor of BET-specific BRD4(BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively), with weak selectivity at CBP BRD with IC50 of 32.7 μM.

(-)-p-Bromotetramisole Oxalate (6-Bromolevamisole oxalate) is a potent and non-specific inhibitor of alkaline phosphatase.