Home Ubiquitin E3 Ligase inhibitor - HIF inhibitor - PROTAC chemical VH298 For research use only.

VH298

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.

VH298 Chemical Structure

VH298 Chemical Structure

CAS: 2097381-85-4

Selleck's VH298 has been cited by 1 publication

Purity & Quality Control

Batch: S844901 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] Insoluble] false Purity: 99.94%
99.94

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Signaling Pathway

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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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Sprague-Dawley rats intraperitoneal injected of streptozotocin at 65 mg/kg
Dosages 30 μM VH298 in PBS (100 microlitres)
Administration local injection

Chemical Information & Solubility

Molecular Weight 523.65 Formula

C27H33N5O4S
CAS No. 2097381-85-4 SDF --
Smiles CC1=C(SC=N1)C2=CC=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)C4(CC4)C#N)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (190.96 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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.

Handling Instructions

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