2. Cell Cycle/DNA Damage Apoptosis
  3. Polo-like Kinase (PLK) Apoptosis
  4. PLK1-IN-16

PLK1-IN-16 is a selective polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.25 nM. PLK1-IN-16 exhibits lower inhibitory potency against PLK2 and PLK3, induces G2 phase cell cycle arrest, induces apoptosis, and exhibits antiproliferative activity against tumor cells. PLK1-IN-16 can be stable under simulated gastric acid environmental conditions, and acceptable CYP 450 inhibition. PLK1-IN-16 can be used for the study of triple-negative breast cancer (TNBC), breast cancer, leukemia.

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

PLK1-IN-16

PLK1-IN-16 Chemical Structure

CAS No. : 3068378-51-5

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

PLK1-IN-16 Related Antibodies

Top Publications Citing Use of Products

View All Polo-like Kinase (PLK) Isoform Specific Products:

View All Isoforms
PLK1 PLK2 PLK3 PLK4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PLK1-IN-16 is a selective polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.25 nM. PLK1-IN-16 exhibits lower inhibitory potency against PLK2 and PLK3, induces G2 phase cell cycle arrest, induces apoptosis, and exhibits antiproliferative activity against tumor cells. PLK1-IN-16 can be stable under simulated gastric acid environmental conditions, and acceptable CYP 450 inhibition. PLK1-IN-16 can be used for the study of triple-negative breast cancer (TNBC), breast cancer, leukemia[1].

IC50 & Target[1]

PLK1

0.25 nM (IC50)

PLK2

15.7 nM (IC50)

PLK3

8.97 nM (IC50)

In Vitro

PLK1-IN-16 (compound B7) inhibits proliferation of MDA-MB-231, MDA-MB-361, and MV-4-11 cells with IC50 values of 72.5 nM, 316 nM, and 32.1 nM respectively[1].
PLK1-IN-16 (12.5-200 nM; 72 h) arrests MV-4-11 cells in the G2 phase in a dose-dependent manner[1].
PLK1-IN-16 (5.0-80.0 nM; 72 h) induces apoptosis in MV-4-11 cells in a dose-dependent manner[1].
PLK1-IN-16 (2 h) is stable under simulated gastric acid conditions with a residual rate of 98.4% after 2 h[1].
PLK1-IN-16 has weak inhibitory effects on CYP1A2, CYP2C9, CYP2C19, and CYP2D6, and strong inhibition of CYP3A4 (IC50 of ~1 μM)[1].
PLK1-IN-16 has high plasma protein binding rates in human (99.6%), rat (99.7%), and mouse (99.4%) plasma[1].

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

PLK1-IN-16 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: MV-4-11
Concentration: 12.5 nM,
25.0 nM, 50.0 nM, 100 nM, and 200 nM
Incubation Time: 72 h
Result: Induced G2 phase arrest in a dose-dependent manner, with 4N DNA aggregation observed starting at 100 nM.

Apoptosis Analysis[1]

Cell Line: MV-4-11
Concentration: 5.0 nM,
10.0 nM, 20.0 nM, 40.0 nM and 80.0 nM
Incubation Time: 72 h
Result: Increased apoptosis rate in a concentration-dependent manner, with rates ranging from 10.98% to 34.09%.
Parmacokinetics
Species Dose Route AUC0-t T1/2 CL MRT0-t Vd Tmax Cmax F
Rat[1] 10 mg/kg i.g. 578 ng·h/mL 2.11 h / 2.48 h / 1.17 h 199 ng/mL 20.1 %
Rat[1] 1 mg/kg i.v. 302 ng·h/mL 0.83 h 56.5 mL/min/kg 0.53 h 2.05 L/kg / / /
In Vivo

PLK1-IN-16 (compound B7) (20 mg/kg; p.o.; once) showed high safety in mice, with normal growth and development and no obvious physiological abnormalities or lesions observed in the heart, liver, spleen, lungs and kidneys[1].

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

526.65

Formula

C26H34N6O4S
CAS No.
SMILES

O=S(N1C2=CC(OC)=C(NC3=NC=C4C(N(C5CCCC5)[C@H](CC)C(N4C)=O)=N3)C=C2CC1)(C6CC6)=O
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PLK1-IN-16 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

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-163068378-51-5Polo-like Kinase (PLK)ApoptosisPLK3MDA-MB-231PLK2MDA-MB-361CYP 450apoptosisPLK1G2 phase cell cycle arrestMV-4-11Polo-like kinase 1Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PLK1-IN-16
Cat. No.:
HY-181051
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.