country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-189208

Copy Link Print Information

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.

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

CAS No.: 902332-77-8
Formula: C₂₇H₂₆N₂O₄
Molecular Weight:442.51

Storage:

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

TopBP1-IN-2 Chemical Structure

CAS No.: 902332-77-8

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Use of MCE Products

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

Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Topoisomerase Isoforms :

In Vitro

ApoptosisAnti-cancerOthers

Apoptosis

Anti-cancer

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].

Anti-cancer

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].

Others

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.

Related Protocols :

Chemical Information

CAS No. 902332-77-8
Molecular Weight 442.51
Formula C₂₇H₂₆N₂O₄
SMILES

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

Handling Instructions (2659 KB)

References

[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

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote