Bioymifi

Bioymifi, a small-molecule death receptor 5 (DR5) agonist, binds to the extracellular domain(ECD) of DR5 with a Kd of 1.2 μM but showed little binding affinity to the DR4 ECD. It induces DR5 clustering and aggregation, leading to apoptosis.

Bioymifi Chemical Structure

Bioymifi Chemical Structure

CAS: 1420071-30-2

Selleck's Bioymifi has been cited by 2 publications

Purity & Quality Control

Batch: S794201 DMSO] 43 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 98%
98

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Biological Activity

Description Bioymifi, a small-molecule death receptor 5 (DR5) agonist, binds to the extracellular domain(ECD) of DR5 with a Kd of 1.2 μM but showed little binding affinity to the DR4 ECD. It induces DR5 clustering and aggregation, leading to apoptosis.
Targets
DR5 receptor [1]
(Cell-based assay)
1.2 μM(Kd)
In vitro
In vitro 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[1].
Cell Research Cell lines Human glioblastoma (T98G) cells
Concentrations 0, 0.3, 1, 3, 10, 30 μM
Incubation Time 48 h
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.

Chemical Information & Solubility

Molecular Weight 494.32 Formula

C22H12BrN3O4S

CAS No. 1420071-30-2 SDF Download Bioymifi SDF
Smiles C1=CC(=CC=C1N2C(=O)C(=CC3=CC=C(O3)C4=CC5=C(C=C4)C(=O)NC5=O)SC2=N)Br
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 43 mg/mL ( (86.98 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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