BU99006 is an irreversible ligand, which binds to subgroup I₂ imidazoline binding proteins. Studies indicate that BU99006 inhibits creatine kinase-B (brain creatine kinase) by covalently binding to Cys283 of the enzymes active site. In addition, BU99006 has been shown to irreversibly inhibit [(3)H]2BFI binding to the active site of I₂ imidazoline. Studies suggest that I₂ imidazoline compounds can partially or fully agonize D2DR (D2-dopamine receptors) with a strength similar to dopamine. BU99006 is a versatile compound that can be ideal in monitoring the function of D2DR and ligand binding in I₂ imidazoline compounds.

An irreversible I₂ imidazoline binding site ligand

Store at 4° C

Solid

2-(Imidazolin-2-yl)-5-isothiocyanatobenzofuran

~1.5 g/cm³ (Predicted)

207.39° C (Predicted)

~432.7° C at 760 mmHg (Predicted)

n²⁰_D 1.74 ± 0.05

Ubiquitin-conjugating enzyme E2 N: IC₅₀ = 4.58 µM (human); Bcl-2-related protein A1: IC₅₀ = 6.11 µM (mouse)

pK_b: 9.29 (Predicted)

Monoamine oxidase A: K_i= 2.3 nM (rat); Monoamine oxidase B: K_i= 2.3 nM (rat); Nischarin: K_i= 2.3 nM (human); Alpha-2a adrenergic receptor: K_i= 16.3 µM (rat)

Soluble in DMSO (10 mg/mL, with heating to 60° C).

MFCD03093194

6603748