2. Immunology/Inflammation
  3. COX
  4. 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.

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SC-58125 Chemical Structure

SC-58125 Chemical Structure

CAS No. : 162054-19-5

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Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target

hCOX-2

0.04 μM (IC50)

hCOX-1

>100 μM (IC50)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SC-58125 Related Antibodies

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.
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].

MedChemExpress (MCE) 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.
Molecular Weight

384.35

Formula

C17H12F4N2O2S
CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

FC(C1=NN(C2=CC=C(S(=O)(C)=O)C=C2)C(C3=CC=C(F)C=C3)=C1)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (650.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6018 mL 13.0090 mL 26.0180 mL
5 mM 0.5204 mL 2.6018 mL 5.2036 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6018 mL 13.0090 mL 26.0180 mL 65.0449 mL
5 mM 0.5204 mL 2.6018 mL 5.2036 mL 13.0090 mL
10 mM 0.2602 mL 1.3009 mL 2.6018 mL 6.5045 mL
15 mM 0.1735 mL 0.8673 mL 1.7345 mL 4.3363 mL
20 mM 0.1301 mL 0.6504 mL 1.3009 mL 3.2522 mL
25 mM 0.1041 mL 0.5204 mL 1.0407 mL 2.6018 mL
30 mM 0.0867 mL 0.4336 mL 0.8673 mL 2.1682 mL
40 mM 0.0650 mL 0.3252 mL 0.6504 mL 1.6261 mL
50 mM 0.0520 mL 0.2602 mL 0.5204 mL 1.3009 mL
60 mM 0.0434 mL 0.2168 mL 0.4336 mL 1.0841 mL
80 mM 0.0325 mL 0.1626 mL 0.3252 mL 0.8131 mL
100 mM 0.0260 mL 0.1301 mL 0.2602 mL 0.6504 mL
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SC-58125 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SC-58125162054-19-5SC58125SC 58125COXCyclooxygenasecyclooxygenase2COX-2antitumoredemainflammatorycancerInhibitorinhibitorinhibit

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