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Art. -Nr.: HY-189208

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TopBP1-IN-2

TopBP1-IN-2 is an inhibitor of the TopBP1 BRCT_7/8 domain, with a pS1159 phosphopeptide competition IC₅₀ of 6 nM. TopBP1-IN-2 also blocks the direct interaction between TopBP1-BRCT_7/8 and the DNA-binding domain of mutp53R273H, exhibiting an IC₅₀ of 25 nM. TopBP1-IN-2 selectively induces cancer cell apoptosis and inhibits their clonogenic formation, with no significant effects on normal cells. TopBP1-IN-2 is applicable in research related to breast cancer and ovarian cancer.

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CAS. Nr.: 902332-77-8
Formel: C₂₇H₂₆N₂O₄
Molecular Weight:442.51

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

TopBP1-IN-2 Chemical Structure

CAS. Nr.: 902332-77-8

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
Chemical Information
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Verweise
Calculators
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Biologische Aktivität

Beschreibung

Alle Topoisomerase Isoform-spezifische Produkte anzeigen :

In Vitro

TopBP1-IN-2 (compound 4B4) (5 μM; 20 h) selectively induces apoptosis in MDA-MB-468 and MDAH-2774 cancer cells, while no cytotoxic effect is observed in untransformed AML12 mouse hepatocytes^[1].
TopBP1-IN-2 (0-2.5 μM; 24 h) inhibits the colony-forming ability of MDA-MB-468 breast cancer cells, with its IC₅₀ falling in the range of 1 to 2.5 μM ^[1].
TopBP1-IN-2 (0.02-0.5 μM; 2 h) potently inhibits the binding of TopBP1-BRCT7/8 to its native pS1159 phosphopeptide substrate in a cell-free in vitro system, with an IC₅₀ of 6 nM^[1].
TopBP1-IN-2 (0.02-0.5 μM; 2 h) is a potent inhibitor of the TopBP1-BRCT7/8 and mutp53R273H protein-protein interaction, with an IC₅₀ of 25 nM in cell-free biochemical assays^[1].

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

Apoptosis Analysis^[1]

Cell Line:

MDA-MB-468, MDAH-2774, and AML12 mouse hepatocyte cells
Concentration:

5 μM
Incubation Time:

20 h
Result:

Induced a pronounced apoptotic response and significantly elevated caspase-3/7 activity in MDA-MB-468 triple-negative breast cancer cells and MDAH-2774 ovarian cancer cells.
Showed no increase in caspase-3/7 activity in nontransformed AML12 mouse hepatocytes.

Cell Proliferation Assay^[1]

Cell Line:

MDA-MB-468 breast cancer cells
Concentration:

0.1, 1 and 2.5 μM
Incubation Time:

24 h
Result:

Inhibited the colony formation ability of MDA-MB-468 breast cancer cells with an IC₅₀ between 1 and 2.5 μM.

Chemical Information

CAS. Nr. 902332-77-8
Molecular Weight 442.51
Formel C₂₇H₂₆N₂O₄
SMILES

COC1=CC=CC=C1N(CC2)CCN2CC(C3=CC(O)=C(C4=CC=CC=C4)C=C3O5)=CC5=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Lin FT, et al. Development of a structurally distinct TopBP1 inhibitor that enhances PARP blockade and reverses osimertinib resistance. Science advances. 2026 Aug 07;12(32):eaeg1996.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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