Bioymifi --- TRAIL Receptor DR5 Activator
Overview | |
Catalog # | bs-60088c-2mg-solid |
Product Name | Bioymifi --- TRAIL Receptor DR5 Activator |
Specifications | |
Storage Buffer | Powder |
Storage Condition | Store in dry, dark place at -20C for 1 year. |
Target | |
Product Information | Molecular Weight: 494.32 Formula: C22 H12 Br N3 O4 S CAS Number: 1420071-30-2 InChi Key: ULBOWKXOFOTCMU-NLDKGBHCSA-N InChi: InChI=1S/C22H12BrN3O4S/c23-12-2-4-13(5-3-12)26-21(29)18(31-22(26)24)10-14-6-8-17(30-14)11-1-7-15-16(9-11)20(28)25-19(15)27/h1-10,24H,(H,25,27,28)/b18-10-,24-22? Smiles: N=C1S/C(=C\C2=CC=C(O2)C2C=C3C(=CC=2)C(=O)NC3=O)/C(=O)N1C1C=CC(Br)=CC=1 Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years |
Description | Bioymifi is a potent and selective small molecule agonist of DR5, identified by a high-throughput chemical screening for compounds that promote cell death in synergy with a small-molecule mimetic of Smac. Bioymifi directly targets DR5, specifically binds the ECD of DR5 (Kd ~1.2 μM), and induces the formation of DR5 aggregates and DR5 activation. Bioymifi induces caspase-8–dependent apoptosis, which occurs through a DR5-dependent extrinsic pathway but independent of TRAIL. Bioymifi is capable of acting as a single agent to induce DR5 clustering and aggregation, leading to apoptosis without the need for a Smac mimetic in a variety of cancer cell lines, even in U2OS and HT29 cell lines. Bioymifi could be a potential lead compound for the development of small-molecule TRAIL mimics targeting DR5 for cancer therapy. |