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BEC hydrochloride

BEC hydrochloride

产品编号 T6779   CAS 222638-67-7
别名: BEC HCl

BEC hydrochloride (BEC HCl) 是一种缓慢结合的竞争性精氨酸酶 II 抑制剂,在 pH 7.5 时 Ki 值为 0.31 μM。它对大鼠 Arginase I 在 0.4 到 0.6 μM 之间。

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BEC hydrochloride Chemical Structure
BEC hydrochloride, CAS 222638-67-7
规格 价格/CNY 货期 数量
1 mg ¥ 279 现货
2 mg ¥ 397 现货
5 mg ¥ 773 现货
10 mg ¥ 1,370 现货
25 mg ¥ 2,660 现货
50 mg ¥ 3,990 现货
100 mg ¥ 5,680 现货
1 mL * 10 mM (in DMSO) ¥ 867 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: BEC hydrochloride (T6779)
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纯度: 99.05%
纯度: 98.65%
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生物活性
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存储 & 溶解度
参考文献
产品描述 BEC hydrochloride (BEC HCl) is a competitive arginase inhibitor, which bind slowly. Ki of BEC HCl is 0.31 μM (pH7.5) for Arginase II, and is 0.4-0.6 μM for rat Arginase I.
靶点活性 Arginase II:0.31 μM(Ki)
体外活性 BEC causes significant enhancement of NO-dependent smooth muscle relaxation. [2] In myocytes, BEC augments Ca(2+)-dependent NOS activity and NO production, and increases basal contractility. [3] BEC also inhibits the proliferation of human pulmonary artery smooth muscle cells by decreasing the expression levels of cyclin D1 and CDK4, increasing the expression of p27, and partly reducing the phosphorylation of Akt and ERK. [5]
体内活性 In mice with allergic inflammation (OVA/OVA), BEC enhances peribronchiolar and perivascular inflammation, leads to enhanced NF-κB DNA binding and NF-κB-dependent inflammatory gene expression, and causes an increase in the content of NOx. [4] In rats with pulmonary arterial hypertension, BEC reduces the right ventricle systolic pressure. [5]
激酶实验 PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ enzyme assays: The inhibition of PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ human recombinant PI3K isoforms is evaluated using a Kinase-Glo Plus Assay Kit. 12 point half-log concentration-response curves with a top concentration of 100 μM are constructed by dispensing DMSO solubilised compounds into white 384-well medium-binding microplates using an Echo 555. 3 μL of the appropriate PI3K? in Tris buffer (50 mM Tris pH7.4, 0.05% CHAPS, 2.1 mM DTT, and 10 mM MgCl2) is added. The plate is covered and allowed to pre-incubate with compound for 20 minutes prior to addition of 3 μL of substrate solution containing PIP2 and ATP. The enzyme reaction is stopped after 80 minutes by the addition of Kinase Glo detection solution. Plates are covered and incubated for 30 minutes at room temperature before the luminescence signal is read using a PHERAstar plate reader. The final concentrations of DMSO, ATP and PIP2 in the assay are 2%, 8 μM, and 80 μM respectively. The final concentrations of PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ are respectively 20 nM, 20 nM, 45 nM and 30 nM. For PI3Kα, PI3Kβ and PI3Kδ the concentration of active enzyme is determined as outlined in the enzyme assay tight binding limit determination section. For PI3Kγ the concentration of enzyme is determined by Bradford assay. IC50 values are calculated using Genedata Screener.
别名 BEC HCl
分子量 229.49
分子式 C5H12BNO4S·ClH
CAS No. 222638-67-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 42 mg/mL (183 mM)

Ethanol: 42 mg/mL (183 mM)

H2O: 41 mg/mL (178.7 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol / H2O 1 mM 4.3575 mL 21.7874 mL 43.5749 mL 108.9372 mL
5 mM 0.8715 mL 4.3575 mL 8.715 mL 21.7874 mL
10 mM 0.4357 mL 2.1787 mL 4.3575 mL 10.8937 mL
20 mM 0.2179 mL 1.0894 mL 2.1787 mL 5.4469 mL
50 mM 0.0871 mL 0.4357 mL 0.8715 mL 2.1787 mL
100 mM 0.0436 mL 0.2179 mL 0.4357 mL 1.0894 mL

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TargetMol Library Books参考文献

1. Colleluori DM, et al. Biochemistry. 2001, 40(31), 9356-9362. 2. Kim NN, et al. Biochemistry. 2001, 40(9), 2678-2688. 3. Steppan J, et al. Proc Natl Acad Sci U S A. 2006, 103(12), 4759-4764. 4. Ckless K, et al. J Immunol. 2008, 181(6), 4255-4264. 5. Jiang W, et al. Mol Med Rep. 2015, 12(3), 4743-4749.
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相关化合物库

该产品包含在如下化合物库中:
抑制剂库 肿瘤免疫治疗小分子化合物库 经典已知活性库 NO PAINS 化合物库 免疫/炎症分子化合物库 已知活性化合物库 共价抑制剂库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

BEC hydrochloride 222638-67-7 Immunology/Inflammation Arginase Inhibitor NF-κB hyperresponsiveness BEC Hydrochloride metaplasia inhibit BEC Arginase-II BEC HCl inflammation CCL20 inhibitor

 

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