An inhibitor of Plk1
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Plk1-IN-4

Item No. 45382

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[2-[[1-[2-(dimethylamino)acetyl]-2,3dihydro-5-methoxy-1H-indol-6-yl]amino]-5-(trifluoromethyl)-4pyrimidinyl]amino]-2-thiophenecarboxylic acid, methyl ester
CAS Number
2622273-55-4
Synonyms
  • Polo-like Kinase 1-IN-4
  • Polo-like Kinase 1 Inhibitor 4
Molecular Formula
C24H25F3N6O4S
Formula Weight
550.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/ml
SMILES
CN(CC(N(CCC1=C2)C1=CC(NC(N=C3NC4=C(C(OC)=O)SC=C4)=NC=C3C(F)(F)F)=C2OC)=O)C
InChi Code
InChI=1S/C24H25F3N6O4S/c1-32(2)12-19(34)33-7-5-13-9-18(36-3)16(10-17(13)33)30-23-28-11-14(24(25,26)27)21(31-23)29-15-6-8-38-20(15)22(35)37-4/h6,8-11H,5,7,12H2,1-4H3,(H2,28,29,30,31)
InChi Key
INSBBZOXHUDXOP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    Plk1-IN-4 is an inhibitor of polo-like kinase 1 (Plk1; IC50 = 0.508 nM in a cell-free assay).1 It inhibits the growth of HepG2 and SMMC-7721 hepatocellular carcinoma cells (IC50s = 11.1 and 70.9 nM, respectively) and induces cell cycle arrest at the G2/M phase and apoptosis in HepG2 cells. Plk1-IN-4 (30 mg/kg) reduces tumor growth in a HepG2 mouse xenograft model. It also has antiplasmodial activity against P. falciparum (EC50 = 2.8 µM).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Deng, Z., Chen, G., Liu, S., et al. Discovery of methyl 3-((2-((1-(dimethylglycyl)-5-methoxyindolin-6-yl)amino)-5-(trifluoro-methyl) pyrimidin-4-yl)amino)thiophene-2-carboxylate as a potent and selective polo-like kinase 1 (PLK1) inhibitor for combating hepatocellular carcinoma. Eur. J. Med. Chem. 206, 112697 (2020).

    2. Bohmer, M.J., Wang, J., Istvan, E.S., et al. Human polo-like kinase inhibitors as antiplasmodials. ACS Infect. Dis. 9(4), 1004-1021 (2023).