| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
DR5 receptor (Kd = 1.2 μM)
Bioymifi targets the death receptor DR5 (TRAIL-R2), a cell surface receptor that mediates TRAIL-induced apoptosis. By binding to DR5, Bioymifi blocks the interaction between TRAIL and DR5, preventing the formation of the death-inducing signaling complex (DISC) and inhibiting the activation of caspase-8 and downstream apoptotic pathways. The compound's antagonism of DR5 makes it a valuable tool for studying the role of DR5 in apoptosis and for investigating TRAIL signaling in cancer cells. |
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| ln Vitro |
In T98G cells, Bioymifi can induce cell death without the assistance of the Smac mimetic. Bioymifi induces the processing of caspase-3 into smaller fragments at a concentration of 10 μM. For bioymifi-induced cell death to occur, caspase-8 and the associated extrinsic apoptotic pathway are necessary. DR5-dependent death pathways are induced by Bioymifi, wholly unaffected by TRAIL. With a Kd of 1.2 μM, Bioymifi binds the DR5 ECD but has low affinity for the DR4 ECD. In buffer solutions, it is not very soluble. By interacting with and facilitating the aggregation of DR5, Bioymifi aids in the promotion of apoptosis. The ability of bioymifi to aggregate DR5 at micromolar concentrations is potent enough to cause apoptosis in a variety of cancer cells[1].
In vitro, Bioymifi is a potent antagonist of DR5 that blocks TRAIL-induced apoptosis in cancer cell lines. It inhibits the binding of TRAIL to DR5, preventing the activation of caspase-8 and downstream apoptotic signaling. In cell-based assays, Bioymifi treatment results in reduced TRAIL-induced cell death, decreased caspase activation, and inhibition of apoptotic markers. The compound's selectivity for DR5 over other TNFR family members is confirmed using selectivity profiling. Bioymifi is a valuable tool for studying DR5 signaling and apoptosis. |
| ln Vivo |
In vivo, Bioymifi has been studied for its potential in cancer research. By blocking DR5 signaling, the compound can inhibit TRAIL-induced apoptosis and modulate tumor progression. Bioymifi has been evaluated in preclinical studies to understand the role of DR5 in cancer biology. Comprehensive in vivo efficacy studies are needed to fully characterize its effects. Bioymifi is a valuable research tool for studying DR5 function.
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| Enzyme Assay |
In vitro receptor binding assays for Bioymifi involve measuring its binding affinity to DR5 (TRAIL-R2). The receptor is incubated with a radiolabeled ligand and varying concentrations of Bioymifi. The displacement of the radiolabeled ligand is measured, and the IC₅₀ or Ki value is calculated. The compound's selectivity for DR5 over other TNFR family members is assessed using similar assays. These assays confirm the compound's mechanism of action as a DR5 antagonist.
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| Cell Assay |
Plotted as a function of A2C2 or bioymifi concentration are the dose-response curves for bioymifi and A2C2 in T98G cells. A2C2 or bioymifi, alone or in combination with 1 μM Smac mimetic (SM), are applied to human glioblastoma (T98G) cells in a range of concentrations for 48 hours. A2C2 or bioymifi-free treatment is used to normalize the corresponding cell survival.
In vitro cell-based assays for Bioymifi evaluate its effects on TRAIL-induced apoptosis. Cancer cells are cultured and treated with TRAIL in the presence or absence of Bioymifi. Apoptosis is quantified by measuring caspase-3/7 activity, by Annexin V staining, or by assessing cell viability using MTT or CellTiter-Glo assays. These assays confirm the compound's functional activity as a DR5 antagonist. |
| Animal Protocol |
In vivo animal experiments for Bioymifi have been conducted in mouse models of cancer. Tumor-bearing mice are treated with Bioymifi, and tumor growth is monitored. The compound's effects on TRAIL-induced apoptosis in tumor tissues are assessed by immunohistochemistry for cleaved caspase-3. Pharmacokinetic studies are conducted to determine the compound's half-life, clearance, and tissue distribution. Comprehensive in vivo studies are ongoing.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) data for Bioymifi are limited. The compound has a molecular weight of 473.54 g/mol. It is soluble in DMSO. The compound's metabolic stability, half-life, and bioavailability have not been fully characterized. Comprehensive ADME studies are needed to fully characterize the pharmacokinetic profile of Bioymifi.
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| Toxicity/Toxicokinetics |
The toxicity profile of Bioymifi has not been extensively characterized. In laboratory settings, Bioymifi should be handled as a hazardous chemical. Appropriate personal protective equipment should be used when handling the compound. The compound is for research use only and is not intended for human or veterinary use. Comprehensive toxicological studies are needed.
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| References | |
| Additional Infomation |
Bioymifi is a small molecule that mimics the tumor necrosis factor-associated apoptosis-inducing ligand (TRAIL). After binding to death receptor 5 (DR5) on cancer cells, Bioymifi may trigger apoptosis via a caspase-dependent pathway. Currently, Bioymifi is being investigated as an anti-tumor drug.
Mechanism of Action In cancer cells, the tumor necrosis factor (TNF)-associated apoptosis-inducing ligand (TRAIL) initiates apoptosis by binding to death receptor 5 (DR5). Conversely, normal cells express high levels of decoy receptors (DcRs), which partially or completely lack the functional death domain (DD). Therefore, the binding of TRAIL to normal cells does not induce cell death. For this reason, small molecules that mimic TRAIL activity may have the potential as chemotherapeutic drugs. Bioymifi mimics the activity of TRAIL; after binding to the extracellular domain (ECD) of DR5, it can induce cancer cell aggregation, leading to apoptosis. Bioymifi is a small-molecule inhibitor that targets the death receptor DR5 (TRAIL-R2). It has a molecular formula of C₂₆H₂₃N₃O₄S and a molecular weight of 473.54 g/mol. Bioymifi is an antagonist of DR5 that blocks the binding of TRAIL to DR5, thereby inhibiting TRAIL-induced apoptosis. The compound has been studied for its potential in cancer research. Bioymifi is a valuable research tool for studying DR5 function and TRAIL signaling. |
| Molecular Formula |
C22H12BRN3O4S
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|---|---|
| Molecular Weight |
494.319
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| Exact Mass |
492.973
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| Elemental Analysis |
C, 53.46; H, 2.45; Br, 16.16; N, 8.50; O, 12.95; S, 6.49
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| CAS # |
1420071-30-2
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| Related CAS # |
1420071-30-2
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| PubChem CID |
70678419
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| Appearance |
Brown to reddish brown solid powder
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| Density |
1.8±0.1 g/cm3
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| Index of Refraction |
1.791
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| LogP |
4.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
31
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| Complexity |
841
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(/C(SC1=N)=C/C2=CC=C(O2)C3=CC(C(N4)=O)=C(C=C3)C4=O)N1C5=CC=C(C=C5)Br
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| InChi Key |
ULBOWKXOFOTCMU-NLDKGBHCSA-N
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| InChi Code |
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?
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| Chemical Name |
5-[5-[(Z)-[3-(4-bromophenyl)-2-imino-4-oxo-1,3-thiazolidin-5-ylidene]methyl]furan-2-yl]isoindole-1,3-dione
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| Synonyms |
Bioymifi
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 12.5~43 mg/mL (25.3~9 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (2.53 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 8.33 mg/mL (16.85 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0230 mL | 10.1149 mL | 20.2298 mL | |
| 5 mM | 0.4046 mL | 2.0230 mL | 4.0460 mL | |
| 10 mM | 0.2023 mL | 1.0115 mL | 2.0230 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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