1. Cell Cycle/DNA Damage Apoptosis
  2. Polo-like Kinase (PLK) Apoptosis
  3. YLT-11

YLT-11 is a potent, selective and orally active PLK4 inhibitor with Kd values of >10000, 653, >10000, 5.2 nM for PLK1, PLK2, PLK3, PLK4, respectively. YLT-11 shows antiproliferative activity. YLT-11 induces Apoptosis and cell cycle arrest at G2/M phase. YLT-11 show anticancer activity.

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YLT-11 Chemical Structure

YLT-11 Chemical Structure

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Description

YLT-11 is a potent, selective and orally active PLK4 inhibitor with Kd values of >10000, 653, >10000, 5.2 nM for PLK1, PLK2, PLK3, PLK4, respectively. YLT-11 shows antiproliferative activity. YLT-11 induces Apoptosis and cell cycle arrest at G2/M phase. YLT-11 show anticancer activity[1].

IC50 & Target[1]

PLK4

5.2 nM (Kd)

PLK2

653 nM (Kd)

PLK1

>10000 nM (Kd)

PLK3

>10000 nM (Kd)

In Vitro

YLT-11 (0-1 µM; 48 h) decreases the expression of p-PLK4 in a dose-dependent manner[1].
YLT-11 (0-0.5 µM; 0-48 h) induces apoptosis and cell cycle arrest at G2/M phase[1].

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

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, MDA-MB-468, BT549, MCF-7 cells
Concentration: 0-10 µM
Incubation Time: 24-96 h
Result: Showed antiproliferative activity in a time-dependent and concentration-dependent manner with IC50s of 120, 68, 73, 74 nM for MDA-MB-231, MDA-MB-468, BT549, MCF-7 cells, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-468, MDA-MB-231 cells
Concentration: 0, 0.25, 0.5, 1 µM
Incubation Time: 48 h
Result: Decreased the expression of p-PLK4 in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-468, MDA-MB-231 cells
Concentration: 0.25 µM
Incubation Time: 0-48 h
Result: Induced cell cycle arrest at G2/M phase.

Apoptosis Analysis[1]

Cell Line: MDA-MB-468, MDA-MB-231 cells
Concentration: 0, 0.125, 0.25, 0.5 µM
Incubation Time: 24, 48 h
Result: Induced apoptosis of cancer cells in a time-dependent and concentration-dependent manner with the expression of cleaved caspase-3 and cleaved PARP1 increased.
In Vivo

YLT-11 (30, 90 mg/kg; p.o.; daily for 20 days) shows anti-cancer activity in mice[1].

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

Animal Model: Six-week-old female BALB/c nude mice[1]
Dosage: 30, 90 mg/kg
Administration: P.o.; daily for 20 days
Result: Remarkably inhibited the growth of tumor xenografts in a dose-dependent manner.
Molecular Weight

412.49

Formula

C24H24N6O

SMILES

CC(NC1=NC=CC(C2=CC3=C(C=C2)C(/C=C/C4=CC=C(CN(C)C)C=C4)=NN3)=N1)=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
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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.

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Product Name:
YLT-11
Cat. No.:
HY-115589
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