Date published: 2026-1-7

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BU99006

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Alternate Names:
2-(Imidazolin-2-yl)-5-isothiocyanatobenzofuran
Application:
BU99006 is an irreversible I2 imidazoline binding site ligand
Molecular Weight:
243.28
Molecular Formula:
C12H9N3OS
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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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 may act 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.


BU99006 References

  1. Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand.  |  Coates, PA., et al. 2000. Bioorg Med Chem Lett. 10: 605-7. PMID: 10741563
  2. 5-Isothiocyanato-2-benzofuranyl-2-imidazoline (BU99006) an irreversible imidazoline(2) binding site ligand: in vitro and in vivo characterisation in rat brain.  |  Tyacke, RJ., et al. 2002. Neuropharmacology. 43: 75-83. PMID: 12213261
  3. Relationship between imidazoline(2) sites and monoamine oxidase.  |  Paterson, LM., et al. 2003. Ann N Y Acad Sci. 1009: 353-6. PMID: 15028610
  4. Initial evaluation of novel selective ligands for imidazoline(2) receptors in rat whole brain.  |  Tyacke, RJ., et al. 2003. Ann N Y Acad Sci. 1009: 357-60. PMID: 15028611
  5. Identification of an I(2) binding protein from rabbit brain.  |  Kimura, A., et al. 2003. Ann N Y Acad Sci. 1009: 364-6. PMID: 15028613
  6. Imidazoline binding sites and their ligands: an overview of the different chemical structures.  |  Dardonville, C. and Rozas, I. 2004. Med Res Rev. 24: 639-61. PMID: 15224384
  7. In vitro and in vivo effect of BU99006 (5-isothiocyanato-2-benzofuranyl-2-imidazoline) on I2 binding in relation to MAO: evidence for two distinct I2 binding sites.  |  Paterson, LM., et al. 2007. Neuropharmacology. 52: 395-404. PMID: 17045310
  8. Modulation of stress by imidazoline binding sites: implications for psychiatric disorders.  |  Smith, KL., et al. 2009. Stress. 12: 97-114. PMID: 19006007
  9. Identification of an imidazoline binding protein: creatine kinase and an imidazoline-2 binding site.  |  Kimura, A., et al. 2009. Brain Res. 1279: 21-8. PMID: 19410564
  10. Novel imidazoline compounds as partial or full agonists of D2-like dopamine receptors inspired by I2-imidazoline binding sites ligand 2-BFI.  |  Giorgioni, G., et al. 2010. Bioorg Med Chem. 18: 7085-91. PMID: 20801048
  11. Behavioral effects of the imidazoline I(2) receptor ligand BU99006 in rats.  |  Qiu, Y., et al. 2014. Behav Pharmacol. 25: 130-6. PMID: 24518265
  12. Dysregulation of IRAS/nischarin and other potential I1-imidazoline receptors in major depression postmortem brain: Downregulation of basal contents by antidepressant drug treatments.  |  Keller, B. and García-Sevilla, JA. 2017. J Affect Disord. 208: 646-652. PMID: 27836117
  13. Effects of I2-imidazoline receptor (IR) alkylating BU99006 in the mouse brain: Upregulation of nischarin/I1-IR and μ-opioid receptor proteins and modulation of associated signalling pathways.  |  Keller, B. and García-Sevilla, JA. 2017. Neurochem Int. 108: 169-176. PMID: 28342965
  14. Morphine Binds Creatine Kinase B and Inhibits Its Activity.  |  Weinsanto, I., et al. 2018. Front Cell Neurosci. 12: 464. PMID: 30559651
  15. A high-throughput screen of pharmacologically active compounds for inhibitors of UHRF1 reveals epigenetic activity of anthracycline derivative chemotherapeutic drugs.  |  Giovinazzo, H., et al. 2019. Oncotarget. 10: 3040-3050. PMID: 31105884

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

BU99006, 5 mg

sc-300307
5 mg
$240.00