H3B-120 | CPS1 Inhibitor | AmBeed-信号通路专用抑制剂

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H3B-120 99%+

货号：A1365561 产品仅供科研

H3B-120 is a highly selective, competitive and allosteric carbamoyl phosphate synthetase 1 (CPS1) inhibitor with an IC50 of 1.5 μM and a Ki of 1.4 μM. H3B-120 has anti-cancer activity[1].

H3B-120 化学结构
CAS号：2194903-42-7

H3B-120 3D分子结构
CAS号：2194903-42-7

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H3B-120 纯度/质量文件

货号：A1365561 标准纯度：99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Mar. Drugs, 2024, 22(5): 194. Ambeed. [ A104599 ]; • Pharmaceuticals, 2024, 17(5): 570. Ambeed. [ A224421 ]; 更多 >

H3B-120 生物活性

描述

Carbamoyl phosphate synthetase 1 (CPS1) catalyzes the first step in the ammonia-detoxifying urea cycle, converting ammonia to carbamoyl phosphate under physiologic conditions. In cancer, CPS1 overexpression supports pyrimidine synthesis to promote tumor growth in some cancer types, while in others CPS1 activity prevents the buildup of toxic levels of intratumoral ammonia to allow for sustained tumor growth. H3B-120 is a highly selective, competitive and allosteric carbamoyl phosphate synthetase 1 (CPS1) inhibitor with an IC50 of 1.5 μM and a Ki of 1.4 μM. H3B-120 has anti-cancer activity. H3B-120 has no inhibition of CPS2 activity of CAD (CPS2, aspartyl transcarbamylase, dihydroorotase). H3B-120 achieves inhibition by binding to an allosteric pocket situated between the integrating and ATP A domains. H3B-120 (25, 50, 75, 100 μM) inhibits urea production in a dose-dependent manner, although the cellular potency decreases significantly compared with enzymatic assays. The half-life of H3B-120 is only 40 min^[1]. Treatment of human hepatocytes with H3B-120 decreased urea release into conditioned media. Stable-isotope tracer experiments using 15N-labeled ammonia in the presence or absence of H3B-120 revealed that H3B120 blocked labeling of pyrimidines but had no effect on purines. H3B-120 could inhibit cellular CPS1 activity related to ammonia conversion to urea and subsequent pyrimidine synthesis^[2].

H3B-120 参考文献

[1]Shihua Yao,et al. Small Molecule Inhibition of CPS1 Activity through an Allosteric Pocket. Cell Chem Biol.2020. 27(3), 259-268.

[2]Ayumu Taguchi,et al. A Promising CPS1 Inhibitor Keeping Ammonia from Fueling Cancer. Cell Chem Biol.2020. 27(3), 253-254.

H3B-120 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.68mL

0.54mL

0.27mL

13.42mL

2.68mL

1.34mL

26.85mL

5.37mL

2.68mL

H3B-120 技术信息

CAS号	2194903-42-7
分子式	C₁₉H₂₄N₄O₂S
分子量	372.485

别名
运输	蓝冰

存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 60 mg/mL(161.08 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

摩尔计算器

计算溶液所需的质量，体积或浓度。 Ambeed 摩尔浓度计算器基于以下方程式：

浓度 (mol/L) × 体积 (L) × 分子量 (g/mol)=质量 (g)

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H3B-120 99%+

H3B-120 纯度/质量文件

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H3B-120 99%+

H3B-120 纯度/质量文件

全球学术期刊中引用的产品

H3B-120 生物活性

H3B-120 参考文献

H3B-120 实验方案

H3B-120 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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