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.
|Cell lines||Human glioblastoma (T98G) cells|
|Preparation method||Dose-response curves of bioymifi and A2C2 in T98G cells are plotted as a function of A2C2 or bioymifi concentration. Human glioblastoma (T98G) cells are treated with various concentrations of A2C2 or bioymifi alone or in combination with 1 μM Smac mimetic (SM) for 48 h. The corresponding cell survival is normalized to the treatment without A2C2 or bioymifi.|
|Concentrations||0, 0.3, 1, 3, 10, 30 μM|
|Incubation time||48 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||43 mg/mL in DMSO|
Small-molecule activation of the TRAIL receptor DR5 in human cancer cells.
Wang G Nat Chem Biol. 2013 Feb;9(2):84-9. PMID: 23292651.
|Related TNF-alpha Products|
Adalimumab is the first fully human, recombinant IgG1 monoclonal antibody that specifically targets human TNF-alpha, MW: 144.19 KD.
Lenalidomide (Revlimid, CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM.
Acetylcysteine(N-acetyl-l-cysteine) is a ROS(reactive oxygen species) inhibitor that antagonizes the activity of proteasome inhibitors. It is also a tumor necrosis factor production inhibitor.
GSK481 is a highly potent and monoselective Receptor Interacting Protein 1 kinase inhibitor.
Necrostatin-1 is a specific RIP1 inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.