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CAS No. 1420071-30-2
Bioymifi, a small-molecule death receptor 5 (DR5) agonist, binds to the extracellular domain(ECD) of DR5 with a Kd of 1.2 μM but showed little binding affinity to the DR4 ECD. It induces DR5 clustering and aggregation, leading to apoptosis.
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|Description||Bioymifi, a small-molecule death receptor 5 (DR5) agonist, binds to the extracellular domain(ECD) of DR5 with a Kd of 1.2 μM but showed little binding affinity to the DR4 ECD. It induces DR5 clustering and aggregation, leading to apoptosis.|
Bioymifi is able to promote cell death without the need for the Smac mimetic in T98G cells. At a 10 μM concentration, bioymifi induces processing of caspase-3 into smaller fragments. Caspase-8 and the related extrinsic apoptotic pathway are essential for bioymifi-induced cell death. Bioymifi induces DR5-dependent death pathways and is independent of TRAIL. Bioymifi binds the ECD of DR5 with a Kd of 1.2 μM but shows little binding affinity to the DR4 ECD. It has poor solubility in buffer solutions. Bioymifi promotes apoptosis by directly binding to and facilitating aggregation of DR5. When bioymifi reaches micromolar concentration, its capability to aggregate DR5 is strong enough to induce apoptosis in various cancer cells.
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