2. MAPK/ERK Pathway Cell Cycle/DNA Damage Apoptosis Autophagy NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. Ribosomal S6 Kinase (RSK) Topoisomerase Apoptosis Autophagy Reactive Oxygen Species (ROS)
  4. RSK2/TOP2-IN-1

RSK2/TOP2-IN-1 is a RSK2/TOP2 dual inhibitor. RSK2/TOP2-IN-1 targets key tumor progression enzymes including ribosomal S6 kinase 2 and topoisomerases IIα/IIβ. RSK2/TOP2-IN-1 shows selectivity index > 2 against all squamous cell carcinoma (SCC) cell lines. RSK2/TOP2-IN-1 can induce cell apoptosis, autophagy and ROS production. RSK2/TOP2-IN-1 can be used for the research of cancer, such as squamous cell carcinoma.

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

RSK2/TOP2-IN-1

RSK2/TOP2-IN-1 Chemical Structure

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RSK2/TOP2-IN-1 Related Antibodies

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Description

RSK2/TOP2-IN-1 is a RSK2/TOP2 dual inhibitor. RSK2/TOP2-IN-1 targets key tumor progression enzymes including ribosomal S6 kinase 2 and topoisomerases IIα/IIβ. RSK2/TOP2-IN-1 shows selectivity index > 2 against all squamous cell carcinoma (SCC) cell lines. RSK2/TOP2-IN-1 can induce cell apoptosis, autophagy and ROS production. RSK2/TOP2-IN-1 can be used for the research of cancer, such as squamous cell carcinoma[1].

IC50 & Target[1]

RSK2

 

topoisomerase II alpha

 

topoisomerase II beta

 

In Vitro

RSK2/TOP2-IN-1 (Compound 7e) (72 h) exerts potent cytotoxicity against oral squamous cell carcinoma (SCC-4, SCC-9, SCC-25) cells with IC50 values of 57.1, 46.5, and 13.0 μM, respectively[1].
RSK2/TOP2-IN-1 (72 h) inhibits colorectal cancer HCT-116, liver cancer HepG2, and melanoma B16-F10 cells with IC50 values of 9.1, 3.4 and 7.5 μM[1].
RSK2/TOP2-IN-1 (500 μM, 24 h) shows <2% hemolysis rate on red blood cells[1].
RSK2/TOP2-IN-1 (93 μM, 24 h) induces apoptosis in SCC-9 cells[1].
RSK2/TOP2-IN-1 (46.5 μM, 48 h) induces LC3-positive autophagic puncta formation in SCC-9-LC3-GFP cells[1].
RSK2/TOP2-IN-1 (93 μM, 24-72 h) induces ROS production in SCC-9 cells[1].
RSK2/TOP2-IN-1 (2.91 μM, 72 h) inhibiting migration in SCC-9 cells, with a 54.7% wound closure rate[1].

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

RSK2/TOP2-IN-1 Related Antibodies

Apoptosis Analysis[1]

Cell Line: SCC-9 cells
Concentration: 93 μM
Incubation Time: 24 h
Result: Activated caspase 3/7 with 78.6% positive cells.
Induced cell shrinkage and membrane blebbing.
In Vivo

RSK2/TOP2-IN-1 (Compound 7e) (100-400 mg/kg, i.p., a single dose) causes no death and no body weight loss in C57BL/6 mice[1].

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

Animal Model: C57BL/6 mice[1]
Dosage: 100, 200 and 400 mg/kg
Administration: Intraperitoneally injection
Result: Caused no death and no body weight loss.
Had no lesions in liver, kidney, heart, or other organs in necropsy.
Had a predicted median lethal dose of 2000 mg/kg.
Molecular Weight

518.64

Formula

C29H26O5S2
SMILES

O=C(C1=CC=CC=C12)C(C(SC3=CC=C(OC)C=C3)C(SC4=CC=C(OC)C=C4)C(C)(C)O5)=C5C2=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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RSK2/TOP2-IN-1 Related Classifications

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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:

RSK2/TOP2-IN-1Ribosomal S6 Kinase (RSK)TopoisomeraseApoptosisAutophagyReactive Oxygen Species (ROS)S6KRSK2TOP2ROSSCCInhibitorinhibitorinhibit

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