Bioymifi, TRAIL Receptor DR5 Activator

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.

Product information

CAS Number: 1420071-30-2

Molecular Weight: 494.32

Formula: C22H12BrN3O4S

Chemical Name: (Z)-5-(5-((3-(4-bromophenyl)-2-imino-4-oxothiazolidin-5-ylidene)methyl)furan-2-yl)isoindoline-1,3-dione

Smiles: N=C1S/C(=C\C2=CC=C(O2)C2=CC3=C(C=C2)C(=O)NC3=O)/C(=O)N1C1C=CC(Br)=CC=1

InChiKey: 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?

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Bioymifi was used at 5-10 µM final concentration in vitro and in cellular assays.

References:

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.

Products are for research use only. Not for human use.