Chemical Structure : PLK1 inhibitor B4
CAS No.:
2991469-28-2
PLK1 inhibitor B4
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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505.51
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Formula
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C24H22F3N3O4S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-(2-(dimethylamino)ethyl)-1,3-dioxo-N-(4-(trifluoromethyl)benzyl)-2,3-dihydro-1H-benzo[de]isoquinoline-6-sulfonamide
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References
1. Li P, et al. Cell Death Dis. 2025 May 12;16(1):374.
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