| Identification | Back Directory | [Name]
S-(2-BORONOETHYL)-L-CYSTEINE HYDROCHLORIDE | [CAS]
222638-67-7 | [Synonyms]
BEC HCl
Reaxys ID: 25974550
S-(2-BORONOETHYL)-L-CYSTEINE HYDROCHLORIDE
BEC hydrochloride - S-(2-Boronoethyl)-L-cysteine hydrochloride
(R)-2-amino-3-((2-boronoethyl)thio)propanoic acid hydrochloride
BEC HCl, 98%, a slow-binding and competitive Arginase II inhibitor | [Molecular Formula]
C5H13BClNO4S | [MDL Number]
MFCD03453539 | [MOL File]
222638-67-7.mol | [Molecular Weight]
229.48 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,Store in freezer, under -20°C | [solubility ]
PBS (pH 7.2): 10 mg/ml | [form ]
A crystalline solid | [color ]
White to yellow |
| Hazard Information | Back Directory | [Description]
BEC is a potent slow-binding competitive inhibitor of recombinant rat liver arginase I with Ki values of 0.4 and 0.6 μM from kinetic analyses. It is also a potent inhibitor of human arginase II with Ki values of 310 and 30 nM at pH 7.5 and 9.5, respectively. It does not inhibit murine iNOS at concentrations up to 1 mM. BEC significantly enhances nitric oxide-dependent relaxation of human penile corpus cavernosum smooth muscle in vitro when used at concentrations ranging from 0.1 to 1 mM. | [Uses]
BEC Hydrochloride is Arginase II inhibitor. For the biological study of the inhibition of arginase II, it prevented nitrate tolerance in human umbilical vein endothelial cell and in mouse aorta. | [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[3]. | 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). |
| [References]
[1] NOEL N. KIM. Probing Erectile Function: S-(2-Boronoethyl)-l-Cysteine Binds to Arginase as a Transition State Analogue and Enhances Smooth Muscle Relaxation in Human Penile Corpus Cavernosum?,?[J]. Biochemistry Biochemistry, 2001, 40 9: 2678-2688. DOI: 10.1021/bi002317h
[2] DIANA M. COLLELUORI David E A. Classical and Slow-Binding Inhibitors of Human Type II Arginase?[J]. Biochemistry Biochemistry, 2001, 40 31: 9356-9362. DOI: 10.1021/bi010783g |
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