HS-173

Catalog No.S7356 Batch:S735601

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Technical Data

Formula

C21H18N4O4S

Molecular Weight 422.46 CAS No. 1276110-06-5
Solubility (25°C)* In vitro DMSO 84 mg/mL (198.83 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.
Targets
PI3Kα [1]
(cell-free assay)
0.8 nM
In vitro

HS-173 shows potent antiproliferative effects in T47D, SK-BR3, and MCF7 cells with IC50 of 0.6, 1.5, and 7.8 μM, respectively. [1] HS-173 causes complete suppression of the PI3K pathway in cancer cell lines (Hep3B and SkBr3). Moreover, HS-173 induces cell apoptosis by affecting cell-cycle distribution and activating caspases, and block VEGF-induced angiogenesis in vitro. [2]

In vivo

HS-173 diminishes blood vessel formation in mice. [2] HS-173 markedly attenuates the development of liver fibrosis by blocking PI3K/Akt signaling in vivo. [4]

Features PI3Kα-selective inhibitor.

Protocol (from reference)

Kinase Assay:

[1]

  • PI3-Kinase assay

    The PI3K assay is performed using the Kinase-Glo Max luminescent kinase assay kit which quantifies the amount of ADP produced by the PI3K reaction. In brief, an active PI3K (100 ng) is preincubated with compound for 5 min in kinase reaction buffer (25 mM MOPS [pH 7.0], 5 mM MgCl2, and 1 mM EGTA) and 10 μg l-α-phosphatidylinositol (PI). Before addition of PI, it is sonicated with sonication buffer (25 mM MOPS [pH 7.0], 1 mM EGTA) in water for 20 min for allowing miscelle formation. Then reaction is started by the addition of 10 μM ATP and ran for 180 min. To terminate kinase reaction, same volume of Kinase-Glo Max buffer is added. After 10 min, the plates are then read on a GloMax plate reader for luminescence detection.

Cell Assay:

[1]

  • Cell lines

    T47D, SK-BR3, MCF7 cells

  • Concentrations

    ~50 μM

  • Incubation Time

    48 hours

  • Method

    Cell viability is performed by a MTT assay. Briefly, T47D cells are plated in 96-well plates for 24 h. Then, the medium is removed and cells were treated with either DMSO as a control or various concentrations of inhibitors. The final concentration of DMSO in the medium was ≤0.1% (v/v). After the cells are incubated for 48 h, 20 μL MTT solution (5 mg/mL) is added to each well for another 4 h at 37 °C. The formazan crystals that formed are dissolved in DMSO (100 μL/well) by constant shaking for 5 min. The plate is then read on a microplate reader at 540 nm. Three replicate wells are used for each analysis. The median inhibitory concentration (IC50, defined as the drug concentration at which cell growth is inhibited by 50%) is assessed from the dose−response curves. To assess the effect of compounds on cell proliferation, T47D cells are cultured with compound (0.1−100 μM) for 48 h before MTT analysis.

Animal Study:

[4]

  • Animal Models

    Male BALB/c mice with CCl4-induced liver fibrosis

  • Dosages

    ~20 mg/kg

  • Administration

    p.o.

Customer Product Validation

, , Cancer Cell Int, 2017, 17:27

Data from [Data independently produced by , , Otorhinolaryngol Head Neck Surg, 2016, 1(2): 44-50.]

Selleck's HS-173 has been cited by 21 publications

Lipophagy-related gene RAB7A is involved in immune regulation and malignant progression in hepatocellular carcinoma [ Comput Biol Med, 2023, 158:106862] PubMed: 37044053
ABCB1 and ABCG2 Overexpression Mediates Resistance to the Phosphatidylinositol 3-Kinase Inhibitor HS-173 in Cancer Cell Lines [ Cells, 2023, 12(7)1056] PubMed: 37048130
The Pro-Fibrotic Response to Lens Injury Is Signaled in a PI3K Isoform-Specific Manner [ Biomolecules, 2022, 12-91181] PubMed: 36139020
Advancement of PI3 Kinase Inhibitor Combination Therapies for PI3K-Aberrant Chordoma [ J Neurol Surg B Skull Base, 2022, 83(1):87-98] PubMed: 35155075
The inhibitors of KDM4 and KDM6 histone lysine demethylases enhance the anti-growth effects of erlotinib and HS-173 in head and neck cancer cells [ Eur J Pharm Sci, 2021, 166:105961] PubMed: 34363938
Soluble Epoxide Hydrolase Inhibitors Regulate Ischemic Arrhythmia by Targeting MicroRNA-1 [ Front Physiol, 2021, 12:717119] PubMed: 34646152
Topical Application of the PI3Kβ-Selective Small Molecule Inhibitor TGX-221 Is an Effective Treatment Option for Experimental Epidermolysis Bullosa Acquisita [ Front Med (Lausanne), 2021, 8:713312] PubMed: 34557502
Topical Application of the PI3Kβ-Selective Small Molecule Inhibitor TGX-221 Is an Effective Treatment Option for Experimental Epidermolysis Bullosa Acquisita [ Front Med (Lausanne), 2021, 8:713312] PubMed: 34557502
Idelalisib Rescues Natural Killer Cells from Monocyte-Induced Immunosuppression by Inhibiting NOX2-Derived Reactive Oxygen Species [ Cancer Immunol Res, 2020, 8(12):1532-1541] PubMed: 32967913
Low dose novel PARP-PI3K inhibition via nanoformulation improves colorectal cancer immunoradiotherapy [ Mater Today Bio, 2020, 8:100082] PubMed: 33294836

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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