2194903-42-7|N1-Benzyl-N1-methyl-N4-(4-methylthiazol-2-yl)piperidine-1,4-dicarboxamide|CsnPharm

CAS No.: 2194903-42-7

H3B-120 Catalog No. CSN26460

Synonyms: H3B-120

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].

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技术信息

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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6847 mL
- 13.4234 mL
- 26.8468 mL
- 5 mM
- 0.5369 mL
- 2.6847 mL
- 5.3694 mL
- 10 mM
- 0.2685 mL
- 1.3423 mL
- 2.6847 mL

技术信息

CAS号	2194903-42-7	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C19H24N4O2S	运输	蓝冰
分子量	372.48	别名	H3B-120

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