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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Polo-like Kinase (PLK)-PLK1 inhibitor B4
PLK1 inhibitor B4

Chemical Structure : PLK1 inhibitor B4

CAS No.: 2991469-28-2

PLK1 inhibitor B4

货号: PC-24600Not For Human Use, Lab Use Only.

PLK1 inhibitor B4 is a novel small molecule inhibitor of polo-like kinase 1 (PLK1) with SPR KD of 5.6 uM, IC50 of 13.52 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PLK1 inhibitor B4 is a novel small molecule inhibitor of polo-like kinase 1 (PLK1) with SPR KD of 5.6 uM, IC50 of 13.52 uM.
B4 inhibits PLK1 phosphorylation as well as decreases the abundance of PLK1 in A549/DDP and A549 cells.
B4 exhibits a potent cytotoxic activity in A549 cells with an IC50 value of 6.8 μM.
B4 specifically binds to PLK1 PBD and inhibits its activity in A549/DDP cells
B4 enhances cisplatin sensitivity in vitro and in vivo by blocking PLK1/PRC1 signaling
B4 (30 mg/kg) exhibits in vivo anticancer activity in an A549/DDP xenograft mice model, combination with cisplatin elicites dramatic regression of drug-resistant tumors.

物理化学性质&存储条件

分子量 505.51
分子式 C24H22F3N3O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(2-(dimethylamino)ethyl)-1,3-dioxo-N-(4-(trifluoromethyl)benzyl)-2,3-dihydro-1H-benzo[de]isoquinoline-6-sulfonamide

参考文献

1. Li P, et al. Cell Death Dis. 2025 May 12;16(1):374.

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