SC-58125

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]. 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 p34^cdc2 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]. 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].