896074-75-2
Chemical Structure
TopBP1-IN-5
- CAS No.: 896074-75-2
- Formula:C21H22N2O3
- Molecular Weight:350.41
IUPAC Name: 6-hydroxy-4-((4-methylpiperazin-1-yl)methyl)-7-phenyl-2H-chromen-2-one
InChIKey: DQTXVFHHDZHPLL-UHFFFAOYSA-N
SMILES: CN1CCN(CC1)CC2=CC(=O)OC3=C2C=C(C(=C3)C4=CC=CC=C4)O
Biological Activity: TopBP1-IN-5 is a TopBP1-BRCT7/8 inhibitor (IC50=2.47-3.8 nM). TopBP1-IN-5 selectively disrupts the interaction of TopBP1-BRCT7/8 with E2F1, mutp53, MIZ1, PLK1, CIP2A, and Top2A, without affecting BRCT1/2- and BRCT5-mediated interactions. TopBP1-IN-5 activates caspase-3/7 and caspase-8 to induce prometaphase arrest, mitotic catastrophe, and apoptosis, while inhibiting the MYC transcriptional program and enhancing the binding of MIZ1 to the p21Cip1 promoter. TopBP1-IN-5 exhibits broad-spectrum anticancer activity in triple-negative breast cancer, ovarian cancer, lung cancer, and acute myeloid leukemia models, and can be used for research on related cancers[1].
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TopBP1-IN-5 | TopBP1-IN-5 is a TopBP1-BRCT7/8 inhibitor (IC50=2.47-3.8 nM). TopBP1-IN-5 selectively disrupts the interaction of TopBP1-BRCT7/8 with E2F1, mutp53, MIZ1, PLK1, CIP2A, and Top2A, without affecting BRCT1/2- and BRCT5-mediated interactions. TopBP1-IN-5 activates caspase-3/7 and caspase-8 to induce prometaphase arrest, mitotic catastrophe, and apoptosis, while inhibiting the MYC transcriptional program and enhancing the binding of MIZ1 to the p21Cip1 promoter. TopBP1-IN-5 exhibits broad-spectrum anticancer activity in triple-negative breast cancer, ovarian cancer, lung cancer, and acute myeloid leukemia models, and can be used for research on related cancers. | |||||||||||||||||||||
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