TopBP1-IN-3
TopBP1-IN-3 is an inhibitor of the TopBP1 BRCT7/8 domain. TopBP1-IN-3 disrupts the BRCT7/8-dependent interactions between TopBP1 and E2F1, mutp53, MIZ1, PLK1, and CIP2A, without affecting its protein binding mediated by other BRCT domains. TopBP1-IN-3 can be used for the research of ovarian cancer and breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 850824-74-7
- Formula: C27H26N2O4
- Molecular Weight:442.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Topoisomerase Isoforms
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Biological Activity
Description
In Vitro
TopBP1-IN-3 (compound 4B5) (5 μM; 20 h) selectively induces apoptosis in MDA-MB-468 triple-negative breast cancer cells and MDAH-2774 ovarian cancer cells, while exhibiting no apoptosis-inducing effect on untransformed AML12 mouse hepatocytes[1].
TopBP1-IN-3 (preincubated at 4°C for 2 h, followed by overnight incubation with the phosphopeptide at 4°C) is a potent inhibitor that blocks the binding of TopBP1-BRCT7/8 to its physiological phosphorylated S1159 peptide ligand, with an IC50 of 8 nM[1].
TopBP1-IN-3 (pre-incubated for 2 h at 4°C, followed by overnight incubation with GST-mutp53R273H (DBD) at 4°C) effectively disrupts the oncogenic protein-protein interaction between TopBP1-BRCT7/8 and mutp53R273H (DBD), with an IC50 of 0.3 μM[1].
TopBP1-IN-3 (0.02-2.5 μM; initial treatment for 24 h, followed by 5 days of culture in compound-free medium) significantly inhibits the long-term clonogenic proliferation capacity of MDA-MB-468 triple-negative breast cancer cells, with its clonogenic survival IC50 falling in the range of 1 to 2.5 μM, which is consistent with that of 4B4[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-468 triple-negative breast cancer cells, MDAH-2774 ovarian cancer cells, nontransformed AML12 mouse hepatocytes
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Concentration:5 μM
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Incubation Time:20 h
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Result:Exert induction of pronounced apoptotic caspase-3/7 activation in MDA-MB-468 and MDAH-2774 cancer cells, and produce no detectable change in caspase-3/7 activity in nontransformed AML12 hepatocytes.
Chemical Information
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CAS No. 850824-74-7
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Molecular Weight 442.51
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Formula C27H26N2O4
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SMILES
OC1=C(C2=CC=CC=C2)C=C(OC(C=C3CN4CCN(C5=CC=C(OC)C=C5)CC4)=O)C3=C1
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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)