BEC HCl

SKU: orb1223180

Description

BEC HCl is a competitive arginase inhibitor, which bind slowly. Ki of BEC HCl is 0.31 μM (pH7.5) for Arginase II, and is 0.4-0.6 μM for rat Arginase I.

Key Properties

• CAS Number: 222638-67-7
• MW: 229.49
• Purity: >98% (HPLC)
• Formula: C₅H₁₂BNO₄S·ClH
• SMILES: C(=O)([C@H](CSCCB(O)O)N)O.Cl
• Target: Antibacterial
• Solubility: H2O : ≥ 35 mg/mL; 152.51 mM

Bioactivity

• In Vivo:
  Administration of the arginase inhibitor BEC decreases arginase activity and causes alterations in NO homeostasis, which are reflected by increases in S-nitrosylated and nitrated proteins in the lungs from inflamed mice. BEC enhances perivascular and peribronchiolar lung inflammation, mucus metaplasia, NF-κB DNA binding, and mRNA expression of the NF-κB-driven chemokine genes CCL20 and KC, and leads to further increases in airways hyperresponsiveness. Animal model: C57BL/6J wild-type mice, mice deficient in arginase 2 (Arg2-/-), mice deficient in both arginase 1 and 2 (Arg1-/-Arg2-/-), and mice deficient in NOX2 (NOX2-/-. Dosage: 20 mg/kg. Administration: I. V. , in 0.9% saline, 1 hour before the injection of LPS. Result: BEC robustly reduced VEGF expression in neuroglia (72% reduction) and macrophage/microglia (87% reduction).
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• In Vitro:
  The X-ray crystal structure of the arginase-BEC complex has been determined at 2.3 resolution from crystals perfectly twinned by hemihedry. The structure of the complex reveals that the boronic acid moiety undergoes nucleophilic attack by metal-bridging hydroxide ion to yield a tetrahedral boronate anion that bridges the binuclear manganese cluster, thereby mimicking the tetrahedral intermediate (and its flanking transition states) in the arginine hydrolysis reaction.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Antibacterial