BEC
(Synonyms: S-(2-硼酸基乙基)-L-半胱氨酸) 目录号 : GC10280
An inhibitor of arginase types I and II
Cas No.:63107-40-4
Sample solution is provided at 25 µL, 10mM.
K(I): 0.4-0.6 microM
S-(2-boronoethyl)-L-cysteine (BEC) is an arginase inhibitor.
Arginases can catalyze the hydrolysis of L-arginine to yield L-ornithine and urea. Recently, studies show that arginases, both the type I and type II isozymes, involve in the regulation of nitric oxide production via modulating the availability of arginine for nitric oxide synthase.
In vitro: Although BEC has been first identified as inhibitor of type I arginase, it was found to be a classical, competitive inhibitor of human type II arginase with K(i) value 0.31 microM at pH 7.5. However, at pH 9.5, BEC was a slow-binding inhibitor of the enzyme with K(i) value 30 nM [1].
In vivo: In animal study, the administration of BEC was found to be able to decrease arginase activity and cause alterations in NO homeostasis, which were indicated by increases in S-nitrosylated and nitrated proteins in the lungs from inflamed mice. Moreover, in contrast to first expectations, BEC could enhance perivascular and peribronchiolar lung inflammation, NF-κB DNA binding, mucus metaplasia, and mRNA expression of the NF-κB-driven chemokine genes including KC and CCL20, and result in further increases in airways hyperresponsiveness [2].
Clinical trial: Up to now, BEC is still in the preclinical development stage.
References:
[1] N. N. Kim, J. D. Cox, R. F. Baggio, 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 40, 2678-2688 (2001).
[2] 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.
Cas No. | 63107-40-4 | SDF | |
别名 | S-(2-硼酸基乙基)-L-半胱氨酸 | ||
化学名 | S-(2-boronoethyl)-L-cysteine | ||
Canonical SMILES | OB(O)CCSC[C@@H](C(O)=O)N | ||
分子式 | C5H12BNO4S | 分子量 | 193.0 |
溶解度 | ≤5mg/ml in PBS(pH7.2) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg |
1 mM | 5.1813 mL | 25.9067 mL | 51.8135 mL |
5 mM | 1.0363 mL | 5.1813 mL | 10.3627 mL |
10 mM | 0.5181 mL | 2.5907 mL | 5.1813 mL |
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工作液浓度: mg/ml;
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >98.00%
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