SC-58125 是一种有效的和选择性的环氧合酶2 (COX-2)的抑制剂，IC50值为 0.04 μM。SC-58125 在体外和体内均表现出抗肿瘤活性，还可以抑制炎症部位的水肿并具有缓解疼痛作用。
| 生物活性 | SC-58125 is a potent and selective inhibitor ofcyclooxygenase 2 (COX-2), with anIC50of 0.04 μM. SC-58125 exhibits antitumor activity in vitro and in vivo. SC-58125 also can inhibit edema at the inflammatory site and has analgesic effect[1][2][3]. |
| IC50& Target | hCOX-2 0.04 μM (IC50) | hCOX-1 >100 μM (IC50) |
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体外研究
(In Vitro) | SC-58125 (0.001-100 μM) has a high degree of selectivity for the inducible form of COX-2 (IC50=1 μM) over the COX-1 (IC50>100 μM)[1].
SC-58125 (10 μM; 20-140 s) is time-dependent and is complete by 1 min, with a half-maximal inhibition at 20 s[1].
SC-58125 (25-100 μM; 3 d) inhibits the in vitro growth of HCA-7 and LLC cells[3].
SC-58125 (100 μM; 12 h) induces G2arrest in LLC cells[3].
SC-58125 (25-100 μM; 3 d) decreases p34cdc2levels in HCA-7 cells[3].
SC-58125 (100 μM; 24 or 72 h) does not induce apoptosis of HCA-7 and LLC cells[3].
Cell Proliferation Assay[3] | Cell Line: | HCA-7 and LLC cells | | Concentration: | 0, 25, 50, 100 μM | | Incubation Time: | 3 days | | Result: | Reduced the cell number and MTT activity in both cell lines in a dose-dependent manner. |
Cell Cycle Analysis[3] | Cell Line: | LLC cells | | Concentration: | 100 μM | | Incubation Time: | 12 hours | | Result: | Increased in the number of cells containing 4n DNA content in a dose- and time-dependent manner.
Reduced the number of mitotic figures. |
Western Blot Analysis[3] | Cell Line: | HCA-7 cells | | Concentration: | 0, 25, 50, 100 μM | | Incubation Time: | 3 days | | Result: | Resulted in a dose-dependent decrease in p34cdc2activity with strong inhibition, even at the lowest concentration. |
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体内研究
(In Vivo) | SC-58125 (10 mg/kg; i.p. every 48 h) inhibits the growth of established colorectal cancer xenografts in mice[3].
SC-58125 (10 mg/kg; a single i.p.) reduces tumor PGE2 levels in mice[3].
SC-58125 (10 mg/kg; a single i.p.) does not change the tumor levels of COX-1 and COX-2 protein in mice[3].
| Animal Model: | Athymic Sprague-Dawley mice are injected HCA-7 cells[3] | | Dosage: | 10 mg/kg | | Administration: | I.p. every 48 h; at the time of tumor implantation or 2 and 4 weeks later | | Result: | Decreased the tumor growth rates significantly. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
