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Sulfathiazole is an orally active, endocrine disruptor targeting the steroidogenic pathway, specifically enhancing the activity of CYP19 in human adrenal cancer cells (H295R) and upregulating the mRN expression of CYP17, CYP19, and 3β-HSD. Sulfathiazole increases the production of 17-estradiol (E2) and has endocrine disrupting effects on aquatic organisms such as the Japanese medaka fish.

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Sulfathiazole Chemical Structure

Sulfathiazole Chemical Structure

CAS No. : 72-14-0

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Based on 3 publication(s) in Google Scholar

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Description

Sulfathiazole is an orally active, endocrine disruptor targeting the steroidogenic pathway, specifically enhancing the activity of CYP19 in human adrenal cancer cells (H295R) and upregulating the mRN expression of CYP17, CYP19, and 3β-HSD. Sulfathiazole increases the production of 17-estradiol (E2) and has endocrine disrupting effects on aquatic organisms such as the Japanese medaka fish[1][2][3].

IC50 & Target

Antibacterial

Cellular Effect
Cell Line Type Value Description References
HepG2 IC50
4161 μM
Compound: 3a
Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay
Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay
[PMID: 22365879]
Sf9 IC50
430 μM
Compound: 19
Inhibition of N-terminal hexa-His tagged human PRMT6 expressed in Sf9 cells using 24 residues of biotin labelled histone4 substrate and tritiated 3H-S-adenosylmethionine by scintillation proximity assay
Inhibition of N-terminal hexa-His tagged human PRMT6 expressed in Sf9 cells using 24 residues of biotin labelled histone4 substrate and tritiated 3H-S-adenosylmethionine by scintillation proximity assay
[PMID: 26824386]
In Vitro

Sulfathiazole (0.02-20 mg/L; 48 h) can significantly increase the production of 17-estradiol (E2), aromatase (CYP19) activity, and mRNA expression of steroidogenesis-related genes such as CYP17, CYP19, and 3βHSD in human adrenal cancer cell (H295R) experiments[1].
Sulfathiazole can effectively inhibit the corrosion of copper in 0.1 M NaCl solution, and the inhibition efficiency can reach more than 80% with increasing concentration[3].

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

Cell Viability Assay[1]

Cell Line: H295R cells
Concentration: 0.2 mg/L, 2 mg/L
Incubation Time: 48 h
Result: Exposure to 0.2 mg/L and 2 mg/L Sulfathiazole for 48 h upregulated the mRNA expression of CYP17, CYP19, and 3βHSD2, which are key genes involved in the steroidogenic pathway.
In Vivo

Sulfathiazole (50 mg/L, 500 mg/L; water exposure; daily feeding; 14 days) significantly increases plasma 17-estradiol (E2) concentrations in male Japanese medaka (Oryzias latipes) models[1].
Sulfathiazole (1%; mixed in purified feed; daily intake) causes a decrease in polymorphonuclear neutrophils, band cells, and metamyelocytes in the bone marrow, necrosis and calcification of skeletal muscle, calcification or hyalinization of pulmonary/coronary/renal arteries, hydropic degeneration and focal hyaline necrosis of hepatocytes, hyaline necrosis of adrenal cortical cells, thyroid hyperplasia, and hemorrhage in subcutaneous tissues, body cavities, and organs in Wistar and Osborne-Mendel albino rat models during and shortly after weaning[2].

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

Animal Model: Male Japanese medaka (Oryzias latipes), 3-4 months old[1]
Dosage: 50 mg/L, 500 mg/L (water)
Administration: Waterborne exposure with ad libitum feeding of Artemia nauplii twice daily, renewed exposure medium at least three times per week for 14 d
Result: After 14-d exposure, plasma E2 concentrations in male medaka were significantly increased to 1.56 ng/mL (50 mg/L) and 2.06 ng/mL (500 mg/L), which were 1.32-fold and 1.75-fold higher than the control (1.18 ng/mL), respectively.
Molecular Weight

255.32

Formula

C9H9N3O2S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(N)C=C1)(NC2=NC=CS2)=O

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 (979.15 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 3.9166 mL 19.5830 mL 39.1659 mL
5 mM 0.7833 mL 3.9166 mL 7.8332 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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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.71%

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 3.9166 mL 19.5830 mL 39.1659 mL 97.9148 mL
5 mM 0.7833 mL 3.9166 mL 7.8332 mL 19.5830 mL
10 mM 0.3917 mL 1.9583 mL 3.9166 mL 9.7915 mL
15 mM 0.2611 mL 1.3055 mL 2.6111 mL 6.5277 mL
20 mM 0.1958 mL 0.9791 mL 1.9583 mL 4.8957 mL
25 mM 0.1567 mL 0.7833 mL 1.5666 mL 3.9166 mL
30 mM 0.1306 mL 0.6528 mL 1.3055 mL 3.2638 mL
40 mM 0.0979 mL 0.4896 mL 0.9791 mL 2.4479 mL
50 mM 0.0783 mL 0.3917 mL 0.7833 mL 1.9583 mL
60 mM 0.0653 mL 0.3264 mL 0.6528 mL 1.6319 mL
80 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2239 mL
100 mM 0.0392 mL 0.1958 mL 0.3917 mL 0.9791 mL
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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.

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Sulfathiazole
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HY-B0507
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