| Molecular Weight: | 494.32 |
| Formula: | C22H12BrN3O4S |
| Purity: | ≥ 97% |
| CAS#: | 1420071-30-2 |
| Solubility: | DMSO up to 50 mM |
| Chemical Name: | (Z)-5-(5-((3-(4-bromophenyl)-2-imino-4-oxothiazolidin-5-ylidene)methyl)furan-2-yl)isoindoline-1,3-dione |
| Storage: | Powder:4oC 1 year. DMSO:4oC3 month;-20oC 1 year. |
Biological Activity:
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.
How to Use:
In vitro:Bioymifi was used at 5-10 µM final concentration in vitro and in cellular assays.
In vivo:n/a
Reference:
- 1. Wang G, et al. Small-molecule activation of the TRAIL receptor DR5 in human cancer cells. (2012) Nat Chem Biol. 9(2):84-89.
Bioymifi_spec.pdf
Bioymifi_MSDS.pdf
Products are for research use only. Not for human use.
