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| Product Name: | J-14 | | Synonyms: | Benzoic acid, 4-[[[4-[4-(2-chlorophenyl)-1-piperazinyl]-6-phenyl-2-pyrimidinyl]thio]methyl]-;4-(((4-(4-(2-Chlorophenyl)piperazin-1-yl)-6-phenylpyrimidin-2-yl)thio)methyl)benzoic acid;cancer,inhibit,damage,Sulfiredoxin,J14,cytotoxicity,Reactive Oxygen Species,J 14,death,adenocarcinoma,Inhibitor,lung,mitochondrial,cells;4-[({4-[4-(2-chlorophenyl)piperazin-1-yl]-6-phenylpyrimidin-2-yl}sulfanyl)methyl]benzoic acid | | CAS: | 1043854-13-2 | | MF: | C28H25ClN4O2S | | MW: | 517.04 | | EINECS: | | | Product Categories: | | | Mol File: | 1043854-13-2.mol |  |
| Boiling point | 762.9±60.0 °C(Predicted) | | density | 1.42±0.1 g/cm3(Predicted) | | storage temp. | Sealed in dry,Room Temperature | | solubility | DMSO: 260 mg/mL (502.86 mM) | | pka | 4.08±0.10(Predicted) | | form | Solid | | color | White to off-white |
| Biological Activity | J14 is a reversible sulfiredoxin inhibitor with IC50 of 8.1 μM. J14 induces oxidative stress (leading to intracellular ROS accumulation) by inhibiting sulfiredoxin, which leads to cytotoxicity and cancer cell death. | | in vitro | J14 (0-100 μM; 0-96 hours; A549 cells) treatment inhibits the growth of A549 cells in a concentration- and a time-dependent manner, and its half inhibitory concentration for the growth of A549 cells was 15.7 μM.
J14 (20 μM; 48-72 hours; A549 cells) treatment causes not only the release of cytochrome c into the cytosol, but also the activation of caspase-3 and caspase-9. J14 induces oxidative damage to mitochondria, resulting in caspase-mediated apoptosis.
J14 treatment significantly increases the accumulation of sulfinic peroxiredoxins and intracellular ROS. Excess accumulation of intracellular ROS causes oxidative damage, leading to cell death. J14 significantly induces cell death in A549 cells in a time-dependent manner, resulting in approximately 40% cell death in 96 hours.
J14 induces oxidative mitochondrial damage and apoptosis. Cell Viability Assay | Cell Line: | A549 cells | | Concentration: | 0-100 μM | | Incubation Time: < /td> | 0 hour, 24 hours, 48 hours, 72 hours, 96 hours | | Result: | Inhibited the growth of A549 cells in a concentration- and a time- dependent manner. | Western Blot Analysis | Cell Line: | A549 cells | | Concentration: | 20 μM | < /tr> | Incubation Time: | 48 hours, 72 hours | | Result: | Caused not only the release of cytochrome c into the cytosol, but also the activation of caspase -3 and caspase-9. | | | in vivo | J14 (50 mg/kg; intraperitoneal injection; daily; for 16 days; BALB/c nude female mice) treatment significantly reduces the average tumor volume. The masses and weights of the primary tumors excised from the J14- | Animal Model: | Six-week-old BALB/c nude female mice injected with A549 cells | | Dosage: | 50 mg/kg | | Administration: | Intraperitoneal injection; daily; for 16 days | | Result: | Significantly reduced the growth of human lung tumor without acute toxicity. | | | target | IC50: 8.1 μM (Sulfiredoxin); ROS |
| | J-14 Preparation Products And Raw materials |
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