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PLK1/BRD4-IN-1

Products Details

Product 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].

Web ID

– HY-143471

Shipping

– Room temperature

Applications

– Cancer-Kinase/protease

Molecular Formula

– C31H43N9O2

References

– [1]Ning-Yu Wang, et al. Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors. Eur J Med Chem. 2020 Apr 1;191:112152.

CAS Number

– 2412707-81-2

Molecular Weight

– 573.73

SMILES

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

Clinical Information

– No Development Reported

Research Area

– Cancer

Solubility

– 10 mM in DMSO

Target

– Apoptosis;Epigenetic Reader Domain;Polo-like Kinase (PLK)

Isoform

– BRD4;PLK1

Pathway

– Apoptosis;Cell Cycle/DNA Damage;Epigenetics

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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