| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
OH14 (75–100 μM; 1 h) enhanced the sensitivity of MCF-7 breast cancer cells and HeLa cells to TNF-related apoptosis-inducing ligand (TRAIL)-induced apoptosis in a dose-dependent manner, as detected by increasing cleaved caspase 3/7 activity and Annexin V staining, respectively [1]. OH14 (100 μM; 1 h) required the R38 residue in cFLIP to enhance the sensitivity of HeLa cells to TRAIL-induced apoptosis, while overexpression of wild-type, H7A, or K18I/R45A mutant cFLIP did not affect this sensitizing activity [1]. OH14 (100 μM; 1 h) significantly enhanced the sensitivity of MCF-7, BT474, and MDA-MB-231 breast cancer cell lines to TRAIL-induced cell death, but its effect on other breast cancer subtypes was not uniform [1]. OH14 (100 μM; 1 h) disrupts TRAIL-mediated recruitment of cFLIP to FADD in HeLa cells, manifested as loss of FRET signaling between cFLIP-YFP and FADD-CFP [1]. OH14 (100 μM; 1 h) specifically disrupts TRAIL-mediated recruitment of cFLIP to the FADD complex in MCF-7 cells, while allowing cleavage and activation of procaspase-8 [1]. OH14 (10 μM; 10 days) enhances the sensitivity of MCF-7 breast cancer cells to TRAIL-induced reduction in colony formation, but does not affect colony growth when used alone [1]. OH14 (10 μM; 24 h) is non-toxic to HEK293 non-neoplastic human embryonic kidney cells, whether used alone or in combination with TRAIL [1].
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| Cell Assay |
Apoptosis Analysis [1]
Cell Types: MCF-7 breast cancer cells, HeLa cells Tested Concentrations: 75 μM, 100 μM Incubation Duration: Pre-incubation for 1 hour, followed by TRAIL treatment for 24 hours Experimental Results: A dose-dependent sensitization effect was observed. The activity of cleaved caspase 3/7 was significantly increased in MCF-7 cells. Annexin V staining was significantly enhanced in HeLa cells. Cell viability assay [1] Cell Types: Breast cancer cell lines: MCF-7, BT474, MDA-MB-231, HCC1954, SUM149 Tested Concentrations: 100 μM Incubation Duration: Pre-incubation for 1 hour, followed by TRAIL treatment for 18 hours Experimental Results: TRAIL significantly enhanced the sensitivity of MCF-7, BT474, and MDA-MB-231 breast cancer cell lines to TRAIL. A similar trend was observed in HCC1954 and SUM149 cells, but the statistical significance was not significant. Western Blot Analysis [1] Cell Types: MCF-7 breast cancer cells Tested Concentrations: 100 μM Incubation Duration: Pre-incubated for 1 hour, followed by TRAIL treatment for 2 hours Experimental Results: TRAIL-induced interaction between FADD and both short and long cFLIP chains was disrupted. FADD interaction with procaspase-8 was not inhibited. The ratio of lysed cFLIP (43 kDa) to unlysed cFLIP (55 kDa) was increased. When used in combination with TRAIL, procaspase-8 was induced to cleave to its active 43 kDa form. |
| References |
| Molecular Formula |
C14H11CL2NO4S
|
|---|---|
| Molecular Weight |
360.21
|
| CAS # |
1018153-87-1
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
CC1=C(C=C(C(S(=O)(NC2=CC=CC=C2C(O)=O)=O)=C1)Cl)Cl
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7762 mL | 13.8808 mL | 27.7616 mL | |
| 5 mM | 0.5552 mL | 2.7762 mL | 5.5523 mL | |
| 10 mM | 0.2776 mL | 1.3881 mL | 2.7762 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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