上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
SC-58125
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。
SC-58125 Chemical Structure
CAS No. : 162054-19-5
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
SC-58125 is a potent and selective inhibitor of cyclooxygenase 2 (COX-2), with an IC50 of 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].
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| IC50 & Target |
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hCOX-2
0.04 μM (IC50)
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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 G2 arrest in LLC cells[3].
SC-58125 (25-100 μM; 3 d) decreases p34cdc2 levels in HCA-7 cells[3].
SC-58125 (100 µM; 24 or 72 h) does not induce apoptosis of HCA-7 and LLC cells[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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 p34cdc2 activity 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].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
| 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.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Gierse JK, et, al. A single amino acid difference between cyclooxygenase-1 (COX-1) and -2 (COX-2) reverses the selectivity of COX-2 specific inhibitors. J Biol Chem. 1996 Jun 28; 271(26): 15810-4.
[2]. Seibert K, et, al. Pharmacological and biochemical demonstration of the role of cyclooxygenase 2 in inflammation and pain. Proc Natl Acad Sci U S A. 1994 Dec 6; 91(25): 12013-7.
[3]. Williams CS, et, al. A cyclooxygenase-2 inhibitor (SC-58125) blocks growth of established human colon cancer xenografts. Neoplasia. Sep-Oct 2001; 3(5): 428-36.
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