| Bioactivity | BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)[1] | ||||||||||||
| Invitro | BRD4/CK2-IN-1 (compound 44e) (0-25 μM; 24 hours) has anti-proliferation effect with IC50s of 2.66 and 3.52 μM in MDA-MB-231 and MDA-MB-468 cells, respectively[1]. BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently induces apoptosis of MDA-MB-231 and MDA-MB-468 cells[1].BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently downregulates Bcl-2 but upregulates Bax and cleaved caspase-3[1].BRD4/CK2-IN-1 (0-10 μM; 24 hours) significantly downregulates the autophagy substrate p62 and up-regulated beclin-1 and LC3II in MDA-MB-231 and MDA-MB[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| Name | BRD4/CK2-IN-1 | ||||||||||||
| CAS | 2756851-99-5 | ||||||||||||
| Formula | C29H30ClN5O5 | ||||||||||||
| Molar Mass | 564.03 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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BRD4/CK2-IN-1
CAS: 2756851-99-5 F: C29H30ClN5O5 W: 564.03
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing pr
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