2. Cell Cycle/DNA Damage
  3. Polo-like Kinase (PLK)
  4. PLK1-IN-4

PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma.

For research use only. We do not sell to patients.

PLK1-IN-4 Chemical Structure

PLK1-IN-4 Chemical Structure

CAS No. : 2622273-55-4

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PLK1-IN-4 Related Antibodies

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Description

PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma[1].

IC50 & Target

IC50:< 0.508 nM (PLK1) [1]
In Vitro

PLK1-IN-4 (compound 31) (0-5 μM; 48 hours) exhibits excellent antiproliferative activities against HCC cells[1].
PLK1-IN-4 (60 and 100 nM; 24 hours) induces abnormal spindle formation in HepG2 and HT-29 cells[1].
PLK1-IN-4 (10-300 nM; 0-48 hours) induces apoptosis in cancer cells through G2/M arrest[1].
PLK1-IN-4 (0-120 nM; 24 hours) increases phosphorylation of PLK1, histone H3 and NPM and decreases phosphorylation of Cdc2 in a dose-dependent manner[1].

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

PLK1-IN-4 Related Antibodies

Cell Proliferation Assay

Cell Line: MDA-MB-231, HeLa, HCT 116, HT-29, HepG2, SMMC7721, A549 ,JeKo-1,K562, Karpas299, A375, DU-145 and L02[1]
Concentration: 0-5 μM
Incubation Time: 48 hours
Result: Exhibited excellent antiproliferative activities against HCC cells, with IC50s of 11.1 nM and 70.9 nM in HepG2 and SMMC7721 cells.

Cell Cycle Analysis

Cell Line: HepG2[1]
Concentration: 10, 30, 60, 100 and 300 nM
Incubation Time: 0, 12, 24, 36 and 48 hours
Result: Induced apoptosis in cancer cells through G2/M arrest.

Western Blot Analysis

Cell Line: HepG2[1]
Concentration: 0, 10, 30, 60, 90 and 120 nM
Incubation Time: 24 hours
Result: Increased phosphorylation of PLK1, histone H3 and NPM and decreased phosphorylation of Cdc2 in a dose-dependent manner.
In Vivo

PLK1-IN-4 exhibits low metabolic stability in species of human, mouse, dog and monkey, with CLhep of 74.3, 330.9, 61.5 and 196.5 mL/min/kg, respectively[1].
PLK1-IN-4 (30 mg/kg; tail vein injection; once or twice daily, for 12 days) suppresses tumor growth in a dose dependent manner[1].
Pharmacokinetic Parameters of PLK1-IN-4 in male ICR mouse[1].

IV (5 mg/kg)
C0 (ng/mL) 1790
T1/2 (h) 1.47
MRT0-inf (h) 0.808
MRT0-t (h) 0.704
AUC0-t (ng·h/mL) 767
AUC0-inf (ng·h/mL) 776
CL (mL/min/kg) 107
VdSS (L/kg) 107

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

Animal Model: Male nu/nu BALB/c mice (4-6 weeks; injected with HepG2 cells)[1]
Dosage: 30 mg/kg
Administration: Tail vein injection; once or twice daily, for 12 days
Result: Suppressed tumor growth in a dose dependent manner, and the tumor growth inhibition (TGI) values were 120.0% and 135.2% at doses of 30 mg/kg once daily and 30 mg/kg twice daily, respectively.
Animal Model: ICR mouse[1]
Dosage: 5 mg/kg
Administration: IV; single (Pharmacokinetics Analysis)
Result: Exhibited a short half-life (T1/2) of 1.47 h, moderate exposure with an area under the curve (AUC0-inf) of 776 ng·h/mL and volume of distribution at steady state (Vdss) of 5.21 L/kg.
Molecular Weight

550.55

Formula

C24H25F3N6O4S
CAS No.
SMILES

COC1=C(C=C2C(CCN2C(CN(C)C)=O)=C1)NC3=NC=C(C(NC4=C(SC=C4)C(OC)=O)=N3)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PLK1-IN-4 Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PLK1-IN-42622273-55-4Polo-like Kinase (PLK)Hepatocellular carcinomaAnticancerSelectiveHepG2Inhibitorinhibitorinhibit

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