2. PI3K/Akt/mTOR Metabolic Enzyme/Protease Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Apoptosis
  3. mTOR Drug Metabolite CDK PPAR Apoptosis
  4. Sulindac sulfone

Sulindac sulfone is an orally active metabolite of Sulindac (HY-B0008). Sulindac sulfone activates PPARγ and drives transcriptional induction of SSAT by binding to the PPRE-2 element. Sulindac sulfone induces Apoptosis. Sulindac sulfone negatively regulates the function of VDAC1/2 to inhibit the mTORC1 pathway, reduces Cyclin D1 levels, and induces G1 cell cycle arrest in colon cancer cells. Sulindac sulfone exerts colon cancer preventive effects through a COX-independent mechanism. Sulindac sulfone can be used in research related to colon cancer.

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Sulindac sulfone

Sulindac sulfone Chemical Structure

CAS No. : 59973-80-7

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Other Forms of Sulindac sulfone:

Sulindac sulfone Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

Sulindac sulfone is an orally active metabolite of Sulindac (HY-B0008). Sulindac sulfone activates PPARγ and drives transcriptional induction of SSAT by binding to the PPRE-2 element. Sulindac sulfone induces Apoptosis. Sulindac sulfone negatively regulates the function of VDAC1/2 to inhibit the mTORC1 pathway, reduces Cyclin D1 levels, and induces G1 cell cycle arrest in colon cancer cells. Sulindac sulfone exerts colon cancer preventive effects through a COX-independent mechanism. Sulindac sulfone can be used in research related to colon cancer[1][2][3].

IC50 & Target[1]

mTORC1

 

PPARγ

 

Cellular Effect
Cell Line Type Value Description References
COLO 320 IC50
> 200 μM
Compound: b
Cytotoxicity against human COLO320 cells after 72 hrs by WST-1 assay
Cytotoxicity against human COLO320 cells after 72 hrs by WST-1 assay
[PMID: 20801552]
MIA PaCa-2 IC50
> 200 μM
Compound: b
Cytotoxicity against human MIAPaCa2 cells after 72 hrs by WST-1 assay
Cytotoxicity against human MIAPaCa2 cells after 72 hrs by WST-1 assay
[PMID: 20801552]
In Vitro

Sulindac sulfone (50-600 μM; 1-6 days) inhibits the proliferation and induces the death of colon cancer cell line Caco-2. After 6 days of treatment, the inhibitory effect on proliferation at concentrations ≥50 μM and the inducing effect on cell death at concentrations ≥150 μM are both statistically significant[1].
Sulindac sulfone (600 μM; duration leading to 50% reduction in colony formation) upregulates the expression of the SSAT gene by 3.94-fold in the colon cancer cell line Caco-2 at its IC50 concentration[1].
Sulindac sulfone (10-600 μM; 24-48 h) induces the expression of SSAT mRNA in the colon cancer cell line Caco-2; at the concentration of 600 μM, the expression level increases by 2.23-fold after 24 h of treatment and by 5.58-fold after 48 h of treatment; statistically significant induction is also observed at concentrations ≥100 μM with 48 h of treatment[1].
Sulindac sulfone (600 μM; 48 h) increases SSAT enzyme activity by 2-fold and reduces intracellular spermine and spermidine levels by 2-fold in human colon cancer Caco-2 cells[1].
Sulindac sulfone (600 μM; 48 h) activates PPAR response elements and increases luciferase activity by 2-fold in Caco-2 colon cancer cells after 48 h of treatment[1].
Sulindac sulfone (up to 10 mM) does not inhibit cyclooxygenase (type I) activity[2].
Sulindac sulfone (1-100 μM) weakly inhibits 5-lipoxygenase activity, with inhibition rates of 10%, 14% and 30% at concentrations of 1 μM, 10 μM and 100 μM, respectively[2].
Sulindac sulfone (1-100 μM) exerts no significant inhibitory effect on 15-lipoxygenase activity: the inhibition rate is 8% at 1 μM, 0% at 10 μM, while the enzyme activity increases by 15% instead at 100 μM[2].
Sulindac sulfone (9.4-600 μM; 72 h) inhibits the growth of colon cancer HT-29, DLD-1 and SW480 cells in a dose-dependent manner. A significant reduction in cell viability is observed at concentrations ≥37.5 μM after 72 h of treatment[3].

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

Sulindac sulfone Related Antibodies

Cell Viability Assay[3]

Cell Line: Colon cancer HT-29, DLD-1, and SW480 cells
Concentration: 9.4, 18.8, 37.5, 75, 150, 300, 600 μM
Incubation Time: 72 h
Result: Inhibited cell growth in all three cell lines in a dose-dependent manner.
Reduced cell viability to ~10-20% at 600 μM across all cell lines.
Caused statistically significant decreases in cell viability at ≥37.5 μM (HT-29), ≥150 μM (DLD-1), and ≥150 μM (SW480).

Cell Cycle Analysis[3]

Cell Line: Colon cancer HT-29, DLD-1, and SW480 cells
Concentration: 75, 150, 300, 600 μM
Incubation Time: 72 h
Result: Induced G1 phase cell cycle arrest in all three cell lines.
Caused statistically significant increases in G1 phase population at all tested concentrations.
Caused statistically significant decreases in S phase population at 300 and 600 μM across all cell lines.

Western Blot Analysis[3]

Cell Line: human colon cancer HT-29, DLD-1, and SW480 cells
Concentration: 600 μM
Incubation Time: 24 h
Result: Did not reduce the expression levels of VDAC1 or VDAC2 in any of the three cell lines.
In Vivo

Sulindac sulfone (500-2000 ppm; dietary; continuous; 31 weeks) inhibits azoxymethane-induced colon carcinogenesis in male F344 rats in vivo in a dose-dependent manner, with the 2000 ppm dose reducing overall colon neoplasia incidence to 26.7% and total tumor multiplicity to 0.43 tumors/animal, without significantly reducing colonic PGE2 levels[2].

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

Animal Model: F344 (male, 6 weeks old at study start, azoxymethane-induced colon cancer model)[2]
Dosage: 500 ppm; 1000 ppm; 2000 ppm
Administration: dietary; continuous; 31 weeks
Result: Achieved mean serum levels of 92 μg/mL (500 ppm), 129 μg/mL (1000 ppm), and 146 μg/mL (2000 ppm), and mean cecal levels of 0.96 mg/mL (500 ppm), 1.24 mg/mL (1000 ppm), and 2.59 mg/mL (2000 ppm), with no metabolic conversion to sulindac or other metabolites detected.
Reduced carcinoma burden to 3.53 cm at 500 ppm (P < 0.05 vs control).
Lowered colon adenoma incidence to 40.0%, carcinoma incidence to 36.7%, and overall neoplasia incidence to 63.3% at 1000 ppm (all P < 0.05 vs control).
Reduced tumor multiplicity to 0.53 adenomas/animal, 0.37 carcinomas/animal, and 0.90 total neoplasia/animal at 1000 ppm (all P < 0.05 vs control).
Lowered tumor burden to 1.50 cm for adenomas, 1.77 cm for carcinomas, and 3.27 cm for total neoplasia at 1000 ppm (all P < 0.05 vs control).
Reduced colon adenoma incidence to 20.0%, carcinoma incidence to 10.0%, and overall neoplasia incidence to 26.7% at 2000 ppm (all P < 0.05 vs control).
Lowered tumor multiplicity to 0.30 adenomas/animal, 0.13 carcinomas/animal, and 0.43 total neoplasia/animal at 2000 ppm (all P < 0.05 vs control).
Reduced tumor burden to 0.70 cm for adenomas, 1.17 cm for carcinomas, and 1.87 cm for total neoplasia at 2000 ppm (all P < 0.05 vs control).
Exhibited a highly significant dose-response relationship for colon tumor incidence (P < 0.0001), multiplicity (P < 0.0001), and burden (P = 0.0001).
Maintained colonic PGE2 levels at 78-118% of control levels across all doses, with no statistically significant reduction detected in either proximal or distal colon.
Molecular Weight

372.41

Formula

C20H17FO4S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O)CC(C1=C/2C=CC(F)=C1)=C(C)C2=C\C3=CC=C(S(=O)(C)=O)C=C3
Shipping

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

DMSO : 125 mg/mL (335.65 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 2.6852 mL 13.4261 mL 26.8521 mL
5 mM 0.5370 mL 2.6852 mL 5.3704 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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In Vivo Dissolution Calculator
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Purity & Documentation

Purity: 98.10%

SDS (393 KB)

COA (256 KB) HNMR (277 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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 2.6852 mL 13.4261 mL 26.8521 mL 67.1303 mL
5 mM 0.5370 mL 2.6852 mL 5.3704 mL 13.4261 mL
10 mM 0.2685 mL 1.3426 mL 2.6852 mL 6.7130 mL
15 mM 0.1790 mL 0.8951 mL 1.7901 mL 4.4754 mL
20 mM 0.1343 mL 0.6713 mL 1.3426 mL 3.3565 mL
25 mM 0.1074 mL 0.5370 mL 1.0741 mL 2.6852 mL
30 mM 0.0895 mL 0.4475 mL 0.8951 mL 2.2377 mL
40 mM 0.0671 mL 0.3357 mL 0.6713 mL 1.6783 mL
50 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3426 mL
60 mM 0.0448 mL 0.2238 mL 0.4475 mL 1.1188 mL
80 mM 0.0336 mL 0.1678 mL 0.3357 mL 0.8391 mL
100 mM 0.0269 mL 0.1343 mL 0.2685 mL 0.6713 mL
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Sulindac sulfone Related Classifications

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  • 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:

Sulindac sulfone59973-80-7mTORDrug MetaboliteCDKPPARApoptosisMammalian target of RapamycinCyclin dependent kinasePeroxisome proliferator-activated receptorsPPARγapoptosisPPRE-2 elementmTORC1 pathwayVDAC1colon cancerSSATCaco-2 human colon cancer cellspolyamineVDAC2Inhibitorinhibitorinhibit

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