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Cat. No. M5272
Bioymifi Structure

DR5 Activator

Size Price Availability Quantity
10mM/1mL In DMSO USD 90 In stock
5mg USD 87 In stock
10mg USD 150 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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 Experiment
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
Animal Experiment
Animal models
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 494.32
Formula C22H12BrN3O4S
CAS Number 1420071-30-2
Purity >98%
Solubility 43 mg/mL in DMSO
Storage at -20°C

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.

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Keywords: Bioymifi, DR5 Activator supplier, TNF-alpha, inhibitors

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