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BEC

Catalog No.GC10280

arginase inhibitor

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BEC Chemical Structure

Cas No.: 63107-40-4

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1mg
$52.00
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5mg
$226.00
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10mg
$398.00
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25mg
$872.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

Cas No. 63107-40-4 SDF
Chemical Name S-(2-boronoethyl)-L-cysteine
Canonical SMILES OB(O)CCSC[C@@H](C(O)=O)N
Formula C5H12BNO4S M.Wt 193
Solubility ≤5mg/ml in PBS(pH7.2) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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