1. Cell Cycle/DNA Damage
  2. Polo-like Kinase (PLK)
  3. ZK-Thiazolidinone

ZK-Thiazolidinone is an ATP-competitive Polo-like kinase 1 (Plk1) inhibitor with an IC50 of 19 nM. ZK-Thiazolidinone inhibits tumor cell proliferation, induces cell cycle arrest and typical mitotic defects. ZK-Thiazolidinone impairs the recruitment of γ-tubulin and Aurora A kinase to centrosomes, resulting in failure of bipolar spindle maintenance and sister chromatid arm cohesion.\nZK-Thiazolidinone is applicable for cancer research.

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ZK-Thiazolidinone

ZK-Thiazolidinone Chemical Structure

CAS No. : 891849-87-9

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Description

ZK-Thiazolidinone is an ATP-competitive Polo-like kinase 1 (Plk1) inhibitor with an IC50 of 19 nM. ZK-Thiazolidinone inhibits tumor cell proliferation, induces cell cycle arrest and typical mitotic defects. ZK-Thiazolidinone impairs the recruitment of γ-tubulin and Aurora A kinase to centrosomes, resulting in failure of bipolar spindle maintenance and sister chromatid arm cohesion.\nZK-Thiazolidinone is applicable for cancer research[1].

In Vitro

ZK-Thiazolidinone (4 d) inhibits the proliferation of various human and mouse tumor cell lines in vitro, with an IC50 value ranging from 0.2 to 1.3 μM[1].
Treatment of HeLa S3 cells with ZK-Thiazolidinone (1 μM; 12 h-48 h) for 12 h induces reversible G2/M cell cycle arrest, whereas prolonged treatment (48 h) leads to cell death; treatment of MCF7 cells with this compound for 24 h under concentration-increasing conditions also induces G2/M arrest[1].
ZK-Thiazolidinone (1 μM; 12 h) induces spindle assembly checkpoint-dependent prometaphase arrest and generates monopolar spindles in HeLa S3 cells[1].
ZK-Thiazolidinone (1 μM; 12 h) disrupts centrosome maturation in HeLa S3 cells by inhibiting the recruitment of γ-tubulin and Aurora A to centrosomes, without altering the localization and related protein levels of Eg5[1].
ZK-Thiazolidinone (1 μM; 0-120 min) disrupts the maintenance of bipolar spindles in metaphase-synchronized HeLa S3 cells, thereby causing spindle collapse into a monopolar spindle array within 120 min[1].
ZK-Thiazolidinone (1 μM; 10-12 h) impairs the stability of K-fibers in HeLa S3 cells and inhibits the separation of sister chromatid arms[1].
ZK-Thiazolidinone (1 μM; 12 h) induces the spreading of Plk1 and PICH along chromatid arms in HeLa S3 cells, and the redistribution of Plk1 requires the involvement of PICH[1].
ZK-Thiazolidinone (1 μM) induces cytokinesis failure in HeLa S3 cells in vitro in a mitotic stage-dependent manner by inhibiting the localization of RhoA and ECT2 to their respective cytokinesis-related sites[1].
ZK-Thiazolidinone (1 μM; 30 min) disrupts the central spindle structure in HeLa cells, inhibits Plk1-dependent phosphorylation and localization of PRC1 and Mklp2, and reduces the interaction between Plk1 and PRC1 in anaphase cells, without altering Aurora B-dependent Mklp1 phosphorylation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: HeLa S3, MCF7
Concentration: 1 μM; increasing concentrations
Incubation Time: 12 h, 24 h, 48 h (1 μM); 12 h (1 μM) followed by 12 h release; 24 h (increasing concentrations)
Result: Induced accumulation of HeLa S3 cells with 4N DNA content (G2/M arrest) and an elevated mitotic index after 12 h treatment with 1 μM; this block was reversed by a 12 h release in fresh medium.
Maintained G2/M arrest after 24 h treatment with 1 μM.
Resulted in an increased proportion of cells with sub-2N DNA content (cell death) after 48 h treatment with 1 μM.
Induced G2/M arrest in both HeLa S3 and MCF7 cells after 24 h treatment with increasing concentrations.
Molecular Weight

493.55

Formula

C23H26F3N5O2S

CAS No.
SMILES

N#CC(C(=O)NCC(F)(F)F)=C1SC(=CNC2=CC=CC(=C2)CCN3CCCC3)C(=O)N1CC

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ZK-Thiazolidinone
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HY-104023
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