| Bioactivity | EZH2/HSP90-IN-29 is a dual inhibitor for EZH2 and HSP90, with IC50s of 6.29 nM and 60.1 nM, for EZH2 and HSP90, respectively. EZH2/HSP90-IN-29 increases apoptosis/necrosis-related gene expression, induces cell cycle arrest at M phase and inhibits reactive oxygen species (ROS) catabolism pathway. EZH2/HSP90-IN-29 is able to cross the blood-brain-barrier (BBB)[1]. |
| Invitro | EZH2/HSP90-IN-29 通过调节 EZH2 和 HSP90 分子伴侣的平衡，抑制 TMZ 耐药胶质母细胞瘤 (GBM) 的增殖 (IC50 为 1.015 μM)[1]。EZH2/HSP90-IN-29 (5 μM) 减少着丝粒蛋白 (CENP)、CDK1 和细胞周期蛋白 B1，从而调节着丝粒组装和有丝分裂，在 M 期阻滞细胞周期[1]。EZH2/HSP90-IN-29 (2 μM) 通过下调 Pt3R 细胞中 RB 结合蛋白 (RBBP8)、BRCA1、DNA 修复和重组蛋白 RAD54B、RAD21以及交叉连接核酸内切酶 EME1 和 BRIP1 的表达来抑制 DNA 修复能力[1]。 EZH2/HSP90-IN-29 (5 μM) 上调 ROS 和裂解 caspase-3 的水平，增加线粒体衍生的 ROS[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> EZH2/HSP90-IN-29 相关抗体: Cell Cytotoxicity Assay[1] Cell Line: |
| In Vivo | EZH2/HSP90-IN-29 (20 mg/kg，腹腔注射，每周两次，共 40 天) 抑制 Pt3R 异种移植 NOD.CB17-Prkdcscid/NCrCrl 小鼠中 Pt3R 诱导的肿瘤生长[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C40H48N4O6 |
| Molar Mass | 680.83 |
| 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]. Sharma S, et al., First-in-Class Dual EZH2-HSP90 Inhibitor Eliciting Striking Antiglioblastoma Activity In Vitro and In Vivo. J Med Chem. 2024 Feb 22;67(4):2963-2985. |