VH298

Catalog No.S8449 Batch:S844901

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Technical Data

Formula

C27H33N5O4S
Molecular Weight 523.65 CAS No. 2097381-85-4
Solubility (25°C)* In vitro DMSO 100 mg/mL (190.96 mM)
Ethanol 100 mg/mL (190.96 mM)
Water 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.)

Preparing Stock Solutions

Biological Activity

Description VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. VH298 blocks the VHL:HIF-α interaction with Kd of 90 nM in isothermal titration calorimetry (ITC) and 80 nM in a competitive fluorescence polarization assay. VH-298 can be used in PROTAC technology.
Targets
VHL:HIF-α [1]
(competitive fluorescence polarization assay)		 VHL:HIF-α [1]
(isothermal titration calorimetry (ITC))
80 nM(Kd) 90 nM(Kd)
In vitro

VH298 can activate the HIF-1 signalling pathway by stabilizing both forms of HIF-1α in vitro. VH298 promotes rFb variability, migration, and synthesis of collagen and regulatory cell factors. VH298 improves the angiogenesis of hUVEC.[2]
In vivo

VH298 can activate the HIF-1 signalling pathway by stabilizing both forms of HIF-1α in vitro. VH298 promotes rFb variability, migration, and synthesis of collagen and regulatory cell factors. VH298 improves the angiogenesis of hUVEC.[2]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    rFb cells, hUVEC cells

  • Concentrations

    10 μM, 30 μM, 100 μM, 200 μM

  • Incubation Time

    48 h

  • Method

    The rFb are trypsinised and placed in flat-bottomed 96-well plates at an initial density of 5000 cells per well. After 24 h of incubation, the medium is changed to VH298-containing medium at different dosages (0 μM, 10 μM, 30 μM, 100 μM, and 200 μM). rFb are incubated at 37°C for 48 h. The proliferation is determined by the Cell Counting Kit-8 (CCK-8) assay. After incubation, rFb are treated with the CCK-8 solution at a final concentration of 10% for 2 h at 37°C, followed by measurement of absorbance at 450nm using a microplate reader.
Animal Study:

[2]
  • Animal Models

    Sprague-Dawley rats intraperitoneal injected of streptozotocin at 65 mg/kg

  • Dosages

    30 μM VH298 in PBS (100 microlitres)

  • Administration

    local injection

Selleck's VH298 has been cited by 1 publication

Design, synthesis, and biological evaluation of first-in-class indomethacin-based PROTACs degrading SARS-CoV-2 main protease and with broad-spectrum antiviral activity [ Eur J Med Chem, 2024, 268:116202] PubMed: 38394929

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.