PLK1-IN-10

CAS: 2991469-21-5 F: C23H22FN3O4S W: 455.50

PLK1-IN-10 (Compound 4Bb) is an orally active PLK1 PBD (polo-box domain) inhibitor. PLK1-IN-10 blocks the interaction of

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Bioactivity	PLK1-IN-10 (Compound 4Bb) is an orally active PLK1 PBD (polo-box domain) inhibitor. PLK1-IN-10 blocks the interaction of PLK1 with the cell division regulator protein 1 (PRC1) and decreases the protein expression of the CDK1-Cyclin B1 complex. PLK1-IN-10 reacts with glutathione (GSH) to increase cellular oxidative stress, ultimately leading to cell death[1].
Invitro	PLK1-IN-10 (0-6 μM; 48 h) 诱导 A549 和 A549/DDP 的细胞周期停滞在 G2/M 期，抑制细胞增殖[1]。PLK1-IN-10 (20 μM) 能够在不同温度范围内稳定 A549/DDP 的 PLK1 蛋白[1]。PLK1-IN-10 (5 μM; 24 h) 与 GSH 反应，产生剂量和时间依赖性的荧光响应，A549/DDP 细胞内荧光强度更高[1]。PLK1-IN-10 (0-9 μM; 48 h) 增加 A549/DDP 胞内 ROS 水平[1]。PLK1-IN-10 (10 μM; 48 h) 抑制 PLK1 与 PRC1 的相互作用，出现多核现象[1]。PLK1-IN-10 对 NCI–H1975 细胞的抗癌活性为 IC50=7.83 μM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PLK1-IN-10 相关抗体: Western Blot Analysis[1] Cell Line:
In Vivo	PLK1-IN-10 (30, 50 mg/kg; i.p.; 每两天一次,持续 32 天) 显著抑制 A549/DDP 耐药异种移植老鼠的肿瘤生长，50 mg/kg 组甚至导致肿瘤回归[1]。PLK1-IN-10 (30 mg/kg; p.o.; 每两天一次,持续 20 天) 有效抑制 NCI–H1975 耐药异种移植老鼠的肿瘤生长[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
CAS	2991469-21-5
Formula	C23H22FN3O4S
Molar Mass	455.50
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]. Li P, Li Y, et al. Identification of naphthalimide-derivatives as novel PBD-targeted polo-like kinase 1 inhibitors with efficacy in drug-resistant lung cancer cells. Eur J Med Chem. 2024 May 5;271:116416.