3h e1s

Manufactured by PerkinElmer

[3H]-E1S is a radiolabeled steroid compound used in research applications. It is a tritium-labeled form of estrone sulfate, a naturally occurring estrogen metabolite. This product is intended for use in appropriate research, development, or testing purposes.

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Lab products found in correlation

3h e217βg, by PerkinElmer (2 mentions) Unlabeled e217βg, by Merck Group (2 mentions) Cck 8, by Merck Group (1 mentions) 3h taurocholic acid, by PerkinElmer (1 mentions) 3h docetaxel, by American Radiolabeled Chemicals (1 mentions) Docetaxel, by LC Laboratories (1 mentions) Triton x 100, by Merck Group (1 mentions) Matrigel, by BD (1 mentions) Fetal bovine serum (fbs), by Cytiva (1 mentions) Rifampicin, by Merck Group (1 mentions) Insulin transferrin selenium, by BD (1 mentions) Dulbecco s modified eagle medium dmem, by Merck Group (1 mentions) Antibiotic antimycotic solution, by Merck Group (1 mentions) Bio safe 2 liquid scintillation mixture, by Research Products International (1 mentions) Dasatinib, by LC Laboratories (1 mentions)

Close spelling variants of this product

[3H]estrone sulfate (E1S) (2 citations)

3 protocols using 3h e1s

Radiolabeled Compounds for Receptor Binding

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[³H]-docetaxel (60 Ci/mmol) and [³H]-xanthine (19.4 Ci/mmol) were purchased from American Radiolabeled Chemicals (St Louis, MO). [³H]-E₂17βG (45 Ci/mmol), [³H]-E₁S (46 Ci/mmol), [³H]-taurocholic acid (5.0 Ci/mmol), and [¹⁴C]-tetraethylammonium (3.2 mCi/mmol) were purchased from PerkinElmer Life and Analytical Sciences (Boston, MA). [³H]-CCK-8 (77 Ci/mmol) was purchased from Amersham Pharmacia Biotech (Buckinghamshire, UK). Unlabeled E₂17βG, E₁S, and CCK-8 were purchased from Sigma-Aldrich (St Louis, MO), and docetaxel was purchased from LC Laboratories (Woburn, MA). All other chemicals were of analytical grade and are commercially available.

Yamada A., Maeda K., Kiyotani K., Mushiroda T., Nakamura Y, & Sugiyama Y. (2014). Kinetic Interpretation of the Importance of OATP1B3 and MRP2 in Docetaxel-Induced Hematopoietic Toxicity. CPT: Pharmacometrics & Systems Pharmacology, 3(7), e126-.

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Radioligand Binding Assay Protocol

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[3H]-E₂17βG (specific activity 41.4 Ci/mmol) and [³H]-E₁S (specific activity 54.0 Ci/mmol) were purchased from Perkin Elmer Life Science (Waltham, MA). Dasatinib and CsA were purchased from LC laboratories (Woburn, MA, USA). Rifampicin, unlabeled E₂17βG, Hanks’ balanced salt solution (HBSS), dimethyl sulfoxide (DMSO), Triton X-100, Dulbecco’s Modified Eagle Medium (DMEM), Dulbecco’s phosphate buffered saline (DPBS), trypsin-EDTA solution, and antibiotic antimycotic solution were purchased from Sigma-Aldrich (St. Louis, MO). Poly-L-lysine was purchased from Trevigen Inc. (Gaithersburg, MD). Geneticin^® (G418), BioCoat^™ culture plates, insulin/transferrin/selenium (ITS⁺), and Matrigel^™ were purchased from BD Biosciences (Bedford, MA). Fetal bovine serum (FBS) was purchased from Hyclone Laboratories (Logan, Utah). Bio-Safe II liquid scintillation mixture was purchased from Research Products International (Mt. Prospect, IL).

Pahwa S., Alam K., Crowe A., Farasyn T., Neuhoff S., Hatley O., Ding K, & Yue W. (2017). Pretreatment with Rifampicin and Tyrosine Kinase Inhibitor Dasatinib Potentiates the Inhibitory Effects toward OATP1B1- and OATP1B3-Mediated Transport without Affecting Plasma Membrane Localization of the Transporters. Journal of pharmaceutical sciences, 106(8), 2123-2135.

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Steroid Sulfatase Inhibition Assay

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For the FP fractions stock, solutions of 25 mg/mL in DMSO were prepared. The crude extract and the fractions were tested at a final concentration of 50 µg/mL. For the isolated compounds, stock solutions of 10 mM in DMSO were prepared. Here, the final test concentration was 20 µM as well as serial dilutions were tested for IC₅₀ determination. STS inhibitory assays were performed as described previously^{34 (link)}. Briefly, a compound’s ability to inhibit STS activity was determined using the lysate of JEG-3, a human placenta choriocarcinoma cell line known to have high STS activity. To determine STS inhibition, activity was measured in the presence of crude extract or fractions using [³H]E₁S (4 × 10⁵ dpm, Perkin Elmer) adjusted to 20 μM with unlabelled E₁S substrate. After incubation of the substrate-fraction with JEG-3 lysate (125 μg of protein/mL) for 1 h, the product formed was isolated from the mixture by extraction with toluene (4 mL), using [4-¹⁴C]E₁ (American Radiolabeled Chemicals) to monitor procedural losses. The positive control for all experiments was 1 µM of STX64 (Irosustat), a potent, selective STS inhibitor^{35 (link)}.

Grienke U., Foster P.A., Zwirchmayr J., Tahir A., Rollinger J.M, & Mikros E. (2019). 1H NMR-MS-based heterocovariance as a drug discovery tool for fishing bioactive compounds out of a complex mixture of structural analogues. Scientific Reports, 9, 11113.

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