1. Cell Cycle/DNA Damage
    Epigenetics
    Apoptosis
  2. Polo-like Kinase (PLK)
    Epigenetic Reader Domain
    Apoptosis
  3. PLK1/BRD4-IN-1

PLK1/BRD4-IN-1 

Cat. No.: HY-143471
Handling Instructions

PLK1/BRD4-IN-1 (9b) is an orally active dual PLK1 and BRD4 inhibitor with IC50 values of 22 nM and 109 nM against PLK1 and BRD4, respectively. PLK1/BRD4-IN-1 induces cell cycle arrest and apoptosis, downregulates the transcription of several proliferation-related oncogenes, and exhibits favorable in vivo antitumor activity.

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

PLK1/BRD4-IN-1 Chemical Structure

PLK1/BRD4-IN-1 Chemical Structure

CAS No. : 2412707-81-2

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Description

PLK1/BRD4-IN-1 (9b) is an orally active dual PLK1 and BRD4 inhibitor with IC50 values of 22 nM and 109 nM against PLK1 and BRD4, respectively. PLK1/BRD4-IN-1 induces cell cycle arrest and apoptosis, downregulates the transcription of several proliferation-related oncogenes, and exhibits favorable in vivo antitumor activity[1].

IC50 & Target

BRD4

109 nM (IC50)

PLK1

22 nM (IC50)

In Vitro

PLK1/BRD4-IN-1 (9b) (72 h) shows broad-spectrum antiproliferative activities[1].
PLK1/BRD4-IN-1 (0-9 µM, 24 h) induces cell cycle arrest[1].
PLK1/BRD4-IN-1 (0-9 µM, 48 h) induces cell apoptosis[1].
PLK1/BRD4-IN-1 inhibits the proliferative of cancer cells by exerting its inhibitory activity on both PLK1 and BRD4[1].

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

Cell Viability Assay[1]

Cell Line: MV4-11, LnCap, HT-29, A375, SKOV-3
Concentration: Cells were maintained in RPMI 1640 or DMEM medium supplemented with 10% FBS (v/v) in 5% CO2, except for MV4-11 cells, which were cultured in IMDM medium.
Incubation Time: 72 h
Result: Showed broad-spectrum antiproliferative activities with IC50 values of 0.13, 0.14, 1.10, 2.82 and 2.51 µM against MV4-11, LnCap, SKOV-3, A375 and HT29 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: MV4-11
Concentration: 0.1, 0.3, 1, 3, 9 µM
Incubation Time: 24 h
Result: Induced obvious G2/M arrest in a concentration-dependent manner

Apoptosis Analysis[1]

Cell Line: MV4-11
Concentration: 0.1, 0.3, 1, 3, 9 µM
Incubation Time: 48 h
Result: Significantly increased the number of Annexin V/PI-positive MV4-11 cells in a concentration-dependent manner.

RT-PCR[1]

Cell Line: MV4-11
Concentration: 0.1, 0.3, 1, 3, 9 µM
Incubation Time: 24 h
Result: Reduced the transcription of c-MYC and MYCN as well as BCL-2, in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: MV4-11
Concentration: 0.1, 0.3, 1, 3, 9 µM
Incubation Time: 48 h
Result: Decreased the expression of c-Myc and Bcl-2 in a concentration dependent-manner and upregulated cleaved caspase-3 and cleaved PARP.
In Vivo

PLK1/BRD4-IN-1 (9b) (60 mg/kg/d; IG; 18 days) results in a significant decrease in average tumor size, with no obvious toxicity[1].

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

Animal Model: Five weeks old male NOD-SCID mice[1].
Dosage: 60 mg/kg/d
Administration: Oral gavage, 18 days; tumor xenograft models were established by subcutaneously injecting 100 µL of 1×108 cell/mL MV4-11 cell suspension into NOD-SCID mice.
Result: Resulted in a significant decrease in average tumor size, with 66% tumor growth inhibition, and didn’t obviously affect the body weight of mice.
Molecular Weight

573.73

Formula

C31H43N9O2

CAS No.
SMILES

O=C(NC1CCN(C)CC1)C2=CC=C(NC(N=C3N(CC4CCCCC4)[[email protected]@H]5CC)=NC=C3N6C5=NN=C6C)C(OC)=C2

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/BRD4-IN-1
Cat. No.:
HY-143471
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