| Bioactivity | NCA029 is a potent and selective homo sapiens caseinolytic protease P (HsClpP) activator with an EC50 of 0.15 μM. NCA029 acts on HsClpP to activate an ATF3-dependent integrative stress response, leading to colon cancer cell death[1]. |
| Invitro | NCA029 抑制人结肠腺癌细胞系 (COAD)，对 HCT116、SW620、HCT15、SW480 和 DLD-1 的 IC50 值分别为 1.1 μM、1.5 μM、3.5 μM、5.4 μM 和 3.1 μM[1] 。NCA029 会导致 HCT116 细胞内 ROS 水平升高，且呈剂量依赖性，表明呼吸链活性受损[1]。NCA029（0.5-2 μM；48 小时）抑制肿瘤细胞增殖和转移[1]。NCA029（0.5-2 μM；48 小时）剂量依赖性地诱导 HCT116 细胞凋亡并将细胞阻滞于 G2/M 期[1]。NCA029 (0.5-2 μM) 剂量依赖性地降低 SDHB 的表达，上调促凋亡蛋白 BAX 的表达，同时下调抗凋亡蛋白 Bcl-2 的表达[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> NCA029 相关抗体: Cell Migration Assay [1] Cell Line: |
| In Vivo | NCA029（1.25-5 mg/kg；静脉注射；每周两次；持续 21 天）显着抑制 HCT116 异种移植物中的肿瘤生长[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C22H20F3N3O |
| Molar Mass | 399.41 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Jiangnan Zhang, et al. Discovery of a Novel Series of Homo sapiens Caseinolytic Protease P Agonists for Colorectal Adenocarcinoma Treatment via ATF3-Dependent Integrated Stress Response. J Med Chem. 2024 Feb 22;67(4):2812-2836. |