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.
- Formula: C29H26O5S2
- Molecular Weight:518.64
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Topoisomerase Isoforms
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Biological Activity
|
RSK2 |
topoisomerase II alpha |
topoisomerase II beta |
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.
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Cell Line:SCC-9 cells
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Concentration:93 μM
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Incubation Time:24 h
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Result:Activated caspase 3/7 with 78.6% positive cells.
Induced cell shrinkage and membrane blebbing.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice[1]
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Dosage:100, 200 and 400 mg/kg
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Administration:Intraperitoneally injection
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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.
Chemical Information
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Molecular Weight 518.64
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Formula C29H26O5S2
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RSK2/TOP2-IN-1 Related Classifications
HY-178029 Related Classifications
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