BEC Hydrochloride
货号:
IB1440
品牌:
Jinpan
暂无详情
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 | 瓶 |
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 |