5.04843

Fbxo3 Inhibitor, BC-1215

• Synonym(s): Fbxo3 Inhibitor, BC-1215, N¹,N²- bis(4-(Pyridin-2-yl)benzyl)ethane-1,2-diamine, F Box Only Protein 3 Inhibitor, F Box Protein 3 Inhibitor, BC1215, F Box and Leucine-rich Repeat Protein 2 Activator, Fbxl2 Activator
• Empirical Formula (Hill Notation): C₂₆H₂₆N₄
• CAS Number: 1507370-20-8
• Molecular Weight: 394.51
• UNSPSC Code: 51111800
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: beige
• solubility: DMSO: 10 mg/mL
• storage temp.: −20°C

Description

General description

A cell-permeable, bis-pyridinylbenzylethanamine that disrupts Fbxo3-Fbxl2 interaction and effectively prevents SCF-Fbxo3-catalyzed Fbxl2 ubiquitination, resulting in cellular Fbxl2 upregulation and thereby SCF-Fbxl2-catalyzed TRAFs (TNF Receptor-Associated Factors) ubiquitination. Effectively reduces cellular TRAFs (5 to 127 µM) and prevents TRAF-mediated cytokines production from LPS-stimulated human PBMC (25 µM). Shown to greatly prevent Cecal Ligation & Puncture-induced plasma cytokine elevation and substantially reduce the severity of lung inflammation post intratracheal P. aeruginosa infection in mice (100 µg/mouse; i.p.) in vivo.

A cell-permeable, bis-pyridinylbenzylethanamine that disrupts Fbxo3-Fbxl2 interaction by targeting Fbxo3 C-terminal ApaG domain and effectively prevents SCF-Fbxo3-catalyzed Fbxl2 ubiquitination, resulting in upregulation of cellular Fbxl2 and thereby SCF-Fbxl2-catalyzed ubiquitination of TRAFs (TNF Receptor-Associated Factors). Effectively reduces cellular TRAFs in human macrophage U937, PBMC, and murine murine MLE cultures (16 to 18 h with 5 to 127 µM BC-1215), resulting in downregulation of TRAF-mediated cytokines production from LPS-stimulated human PBMC (2 µg/mL LPS; 25 µM BC-1215;16 h). Intraperitoneal injection in mice in vivo (100 µg/mouse) is shown to greatly prevent circulating proinflammatory cytokines increase post CLP (Cecal Ligation & Puncture) and substantially reduce the severity of cell infiltration in lung after intratracheal P. aeruginosa PA103 infection.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Fbox3

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Chen, B.B., et al. 2013. Nat. Immunol.14, 470.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable