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VH298 E3 Ligase inhibitor

Name: VH298
Brand: Selleck Chemicals
SKU: S8449
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S8449

VH298 is a potent VHL (Von Hippel-Lindau, the E3 ligase) inhibitor that stabilizes HIF-α. This compound 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. It can be used in PROTAC technology.

Chemical Structure

Molecular Weight: 523.65

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.94

Related Targets	Proteasome E1 Activating DUB p97 SUMO E2 conjugating
Other E3 Ligase Inhibitors	Skp2 inhibitor C1 (SKPin C1) Iberdomide (CC-220) PRT4165 Avadomide (CC-122) Apcin SZL P1-41 Mezigdomide (CC-92480) Homo-PROTAC cereblon degrader 1 MRT-2359 SMER3

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (190.96 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.55mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.625mg/ml (1.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.

Chemical Information, Storage & Stability

Molecular Weight	523.65	Formula	C₂₇H₃₃N₅O₄S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2097381-85-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Mechanism of Action

Targets/IC₅₀/Ki	VHL:HIF-α (competitive fluorescence polarization assay) 80 nM(Kd) VHL:HIF-α (isothermal titration calorimetry (ITC)) 90 nM(Kd)
In vitro	VH298 can activate the HIF-1 signalling pathway by stabilizing both forms of HIF-1α in vitro. This compound promotes rFb variability, migration, and synthesis of collagen and regulatory cell factors. It improves the angiogenesis of hUVEC.
In vivo	VH298 can activate the HIF-1 signalling pathway by stabilizing both forms of HIF-1α in vitro. This compound promotes rFb variability, migration, and synthesis of collagen and regulatory cell factors. It improves the angiogenesis of hUVEC.
References	[1] https://pubmed.ncbi.nlm.nih.gov/27811928/ [2] https://pubmed.ncbi.nlm.nih.gov/30911550/

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