2. Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. Apoptosis Polo-like Kinase (PLK) Epigenetic Reader Domain
  4. PLK1/BRD4-IN-5

PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3  nM and 60.8  nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research.

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

PLK1/BRD4-IN-5 Chemical Structure

PLK1/BRD4-IN-5 Chemical Structure

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PLK1/BRD4-IN-5 Related Antibodies

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Description

PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3  nM and 60.8  nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research[1].

IC50 & Target

PLK1

0.3 nM (IC50)

BRD4

60.8 nM (IC50)

In Vitro

PLK1/BRD4-IN-5 (Compound SC10) shows significant anti-proliferation activity against all three tumor cell lines (MDA-MB-231 IC50 = 17.3  nM, MDA-MB-361 IC50 = 8.4  nM, MV4-11 IC50 = 5.4  nM)[1].

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

PLK1/BRD4-IN-5 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.675 nM, 1.35 nM, 2.7 nM, 5.4 nM and 10.8 nM
Incubation Time: 72 h
Result: Exhibited an increasing rate of apoptosis ranging from 6.65 to 58.35 % in a concentration-dependent manner.
In Vivo


Pharmacokinetic parameters of compounds in Sprague-Dawley Rats [1]

Route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng•h/mL) Cl (mL•min/kg) MRT0-t (h) Vdss (L/kg) F (%)
i.g. 10 3.75 2.00 108 657 / 5.26 / 21.4
i.v. 1 4.9 / / 303 53.6 4.39 16.4 /

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

576.73

Formula

C31H44N8O3
SMILES

CC[C@@H]1C(N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C5C(CCN5C(CN6C[C@@H](N[C@@H](C6)C)C)=O)=C4)OC)C)=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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PLK1/BRD4-IN-5 Related Classifications

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

Keywords:

PLK1/BRD4-IN-5ApoptosisPolo-like Kinase (PLK)Epigenetic Reader DomainDihydropteridone derivativesIsoindolin-1-one or isoindoline moietiesMV4-11 cellsInhibitorinhibitorinhibit

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