| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
Cell experiment: | Cell viability is evaluated via MTT assay. Cells (2×103 HEK-293 cells/well and 3×103 SW-839 cells/well) in 100 μL medium are seeded into 96-well plates, and incubated for 12 h. Next, the medium in each well is replaced with medium containing various concentrations of Chelerythrine Chloride, and the cells are incubated at 37℃ for an additional 24 and 48 h. Subsequently, 20 μL MTT (5 mg/mL) is added to each well. Following an additional incubation at 37℃ for 4 h, the supernatant is removed, and 100 μL DMSO is added to each well. The absorbance values (read at 540 nm) are determined using the iMark(TM) Microplate Absorbance Reader. The data are analyzed using Microplate Manager software (ver. 6.3; 1689520). |
Animal experiment: | A total of 5×106 SW-839 cells are mixed with Matrigel(R), and injected subcutaneously into the flanks of 14 5-week-old male BALB/c nude mice. The mice are maintained in 18×30-cm cages containing three mice each, at a temperature of 22℃ using a 12 h light/dark cycle. Food and water is available ad libitum. The mice are randomLy divided into two groups (n=7). As previously described, the mice are administrated with chelerythrine chloride at a dose of 5 mg/kg/day via intraperitoneal injection for 5 weeks, with the first injection of chelerythrine chlorideurring 24 h after injection with the SW-839 cells. The control mice are administered with the same volume of PBS containing 1% DMSO. The volume and weight of the mouse tumors are measured once a week. All the mice are sacrificed 36 days subsequent to inoculation of the cancer cells, when the tumors are resected. |
| 产品描述 | Chelerythrine is a potent, selective antagonist of PKC (protein kinase C) with IC50 value of 0.66 μM.[1] The alkaloid chelerythrine is a highly specific inhibitor that acts at the regulatory domain of the kinase.[2] It is also a competitive inhibitor with respect to the phosphate acceptor and a non-competitive inhibitor with respect to ATP.[1] Chelerythrine induced a dose-dependent decrease in the cell viability with IC50 value of 2.6 μM measured by MTT reduction assay.[3] Chelerythrine is also a selective and strong inhibitor of Bcl-xL functions and induced cell death in MEF cells with IC50 value of 1.1 μM.[4] Chelerythrine activated MEKK1- and MKK4-dependent JNK1 and p38 pathways then mediated the induction of apoptosis.[5] Chelerythrine stimulated apoptosis in the in vivo rat experiments (5 mg/kg) by inducing the generation of reactive oxygen species.[6] Chelerythrine also has widespread physiological effects on primarily antimicrobial and anti-inflammatory. References: |
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