HS-173

Catalog No.S7356

HS-173 Chemical Structure

Molecular Weight(MW): 422.46

HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.

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2 Customer Reviews

  • b, d Serum-deprived MG-63 (b) and U20S cells (d) were pre-treated with 1 nmol/L HS-173 (PI3Kα inhibitor), 10 nmol/L TGX-221 (PI3Kβ inhibitor), 10 nmol/L CZC24832 (PI3Kγ inhibitor) and 10 nmol/L CAL-101 (PI3Kδ inhibitor) for 1 h, then were incubated with 100 ng/mL Wnt5a and harvested at 30 min after the start of Wnt5a treatment. Data were presented as mean ± SD of 3 determinations. The relative RhoA activity was normalized to the average value of each inhibitor-untreated group

    Cancer Cell Int, 2017. HS-173 purchased from Selleck.

    Western blot analysis of PI3K and Ras-MEK-ERK pathway activation in UM-SCC-1 (B), 2 (C), 14A (D), 69 (E), 92 (F), and 108 (G) following treatment with HS-173 or BKM120.

    Otorhinolaryngol Head Neck Surg, 2016, 1(2): 44-50.. HS-173 purchased from Selleck.

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.
Features PI3Kα-selective inhibitor.
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] Combined treatment with Sorafenib and HS-173 has a synergistic anti-cancer effect on pancreatic cancer cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
T47D cells NFrsSZBEgXSxdH;4bYNqfHliYYPzZZk> MVG0PEBp NWPxXnh[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXDR5RDDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvPiEQvF2= M165TlIyOzh6MUSx
SK-BR-3 cells NV;NNmZ[S3m2b4TvfIlkcXS7IHHzd4F6 M4jr[VQ5KGh? MknCR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2suSlJvMzDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEvPSEQvF2= MUKyNVM5QDF2MR?=
MCF7 cells NGDYVopEgXSxdH;4bYNqfHliYYPzZZk> NITVNHk1QCCq NVK5UGRVS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVcvQCEQvF2= NXvnW3BpOjF|OEixOFE>

... Click to View More Cell Line Experimental Data

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]

Protocol

Kinase Assay:[1]
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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 Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: Male BALB/c mice with CCl4-induced liver fibrosis
  • Formulation: Dissolved in DMSO, and then mixture (DMSO:PEG400:D.W. = 1:5:4).
  • Dosages: ~20 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 84 mg/mL warmed (198.83 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 422.46
Formula

C21H18N4O4S

CAS No. 1276110-06-5
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID