BEC Hydrochloride

BEC Hydrochloride

货号:
IB1440

品牌:
Jinpan

BEC Hydrochloride

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产品简介
有效期 2年
描述 是一个竞争性的 Arginase II抑制剂。
MDL MFCD03453539
别名 S-(2-硼酸基乙基)-L-半胱氨酸盐酸盐
CAS 222638-67-7
分子式 C5H12BNO4S·HCl
分子量 229.48
储存条件 -20℃
纯度 ≥98%
外观(性状) White to Yellow Solid
单位
生物活性 BEC hydrochloride is a slow-binding and competitive Arginase II inhibitor with Ki of 0.31 μM and 30 nM at pH 7.5 and pH 9.5, respectively[1].
IC50 Ki: 0.31 μM (BEC hydrochloride, at pH 7.5) and 30 nM (BEC hydrochloride, at pH 9.5)[1]
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[2].
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].
SMILES N[C@@H](CSCCB(O)O)C(O)=O.[H]Cl
靶点 Arginase
数据来源文献 [1]. Colleluori DM, et al. Classical and slow-binding inhibitors of human type II arginase. Biochemistry. 2001 Aug 7;40(31):9356-62.
[2]. Kim NN, et al. 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. Biochemistry. 2001 Mar 6;40(9):2678-88.
[3]. Ckless K, et al. Inhibition of arginase activity enhances inflammation in mice with allergic airway disease, in association with increases in protein S-nitrosylation and tyrosine nitration. J Immunol. 2008 Sep 15;181(6):4255-64.
规格 2mg 5mg