VH-298

Name: VH-298
Brand: MedChemExpress
SKU: HY-100947
Rating: 5.0 (17 reviews)

Cat. No.: HY-100947 Purity: 99.54%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a K_d value of 80 to 90 nM. VH-298 leads to HIF-α accumulation inside HeLa cells. VH-298 is an E3 ligase Ligand, and can be used for synthesis of PROTACs.

For research use only. We do not sell to patients.

CAS No. : 2097381-85-4

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of VH-298:

cis VH-298 In-stock
VH-298 (Standard) Get quote

17 Publications Citing Use of MCE VH-298

Cell Proliferation/Viability Assay

Bio/Physico-chemical Assay

: VH-298 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2023 May;44(5):940-953. [Abstract]; Quantification of cell viability in the MPP⁺-induced injury model preincubated with VH298 (0-2.5 μM, pre-incubate for 1 hour).

: VH-298 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2023 May;44(5):940-953. [Abstract]; Quantification of ADE neurodegeneration in L4-stage wild-type C. elegans treated with VH298, FG-4592 and Compound 15i prior to exposure to MPP⁺ (1 mM).

: VH-298 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2023 May;44(5):940-953. [Abstract]; Quantification of ADE neurodegeneration in L4-stage nduf-7 (et19) mutants of C. elegans treated with VH298, FG-4592 and Compound 15i. Data are the mean ± SEM; n = 6 plates (20-35 worms per plate); statistical significance was determined by using one-way ANOVA followed by Tukey’s correction.

: VH-298 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2023 May;44(5):940-953. [Abstract]; Representative immunoblots of TH and β-actin from differentiated SH-SY5Y cells transfected with mutant plasmid pcDNA3.1(+)-NDUFS7 Q208STOP and further incubated with VH298 (0.625 μM) for 48 h.

: VH-298 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Jun 16;12(7):621. [Abstract]; Caki-2 cells were treated with VHL inhibitor, VH-298 (50 µM), for 24 h followed by western blot. Densitometric analyses of HIF-1α/HO-1 are shown on the right panel.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Ligands for E3 Ligase Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) MDM2 Cereblon IAP KLHDC2 Fbxo3 RNF4 DCAF11 DCAF1 UHRF1 TRIM21 NEURL1B

View All HIF/HIF Prolyl-Hydroxylase Isoform Specific Products:

View All Isoforms

HIF-1α HIF

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

VHL

Cellular Effect

Cell Line	Type	Value	Description	References
DB	IC₅₀	> 10 μM Compound: VH298	Cytotoxicity against human DB cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human DB cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
HEL	IC₅₀	> 10 μM Compound: VH298	Cytotoxicity against human HEL cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human HEL cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
JJN-3	IC₅₀	> 10 μM Compound: VH298	Cytotoxicity against human JJN-3 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human JJN-3 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
K562	IC₅₀	> 10 μM Compound: VH298	Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human K562 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
MOLM-13	IC₅₀	> 10 μM Compound: VH298	Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
NCI-H929	IC₅₀	> 10 μM Compound: VH298	Cytotoxicity against human NCI-H929 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human NCI-H929 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
RPMI-8226	IC₅₀	> 10 μM Compound: VH298	Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
SU-DHL-6	IC₅₀	> 10 μM Compound: VH298	Cytotoxicity against human SU-DHL-6 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human SU-DHL-6 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]
SUD4	IC₅₀	> 10 μM Compound: VH298	Cytotoxicity against human SU-DHL-4 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay Cytotoxicity against human SU-DHL-4 cells assessed as reduction in cell viability measured after 96 hrs in presence of TNF-alpha by CellTiter-Glo luminescent assay	[PMID: 36996313]

In Vitro

VH-298 is a potent, cell permeable and non-toxic chemical probe that triggers the hypoxic response by blocking the VHL. VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with K_d values of 90 and 80 nM in isothermal titration calorimetry and competitive fluorescence polarization assay. VH-298 binds with VHL complex very fast and dissociates slowly. VH-298 at 50 μM concentration exhibits negligible off-target effects in vitro against more than 100 tested cellular kinases, GPCRs and ion channels. VH-298 is cell permeable and not toxic to cells. The measured permeability of VH-298 is found to be 19.4 nm s ^-1. VH-298 induces concentration- and time-dependent on-target specific accumulation of hydroxylated HIF-α in human cell lines, including HeLa cancer cells and renal cell carcinoma 4 (RCC4) cells. VH-298 increases mRNA levels of EPO by 2.5-fold in RCC4-HA-VHL, but not in VHL-null RCC4-HA, indicating that pharmacological inhibition of VHL is able to stimulate endogenous EPO synthesis. VH-298 proves as effective as hypoxia in raising PHD2 and HK2 protein levels, however in HFF the BNIP3 protein level increases more with VH-298 treatment than hypoxia treatment^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

523.65

Formula

C₂₇H₃₃N₅O₄S

CAS No.

2097381-85-4

Appearance

Solid

Color

Off-white to pink

SMILES

O=C([C@H]1N(C([C@H](C(C)(C)C)NC(C2(CC2)C#N)=O)=O)C[C@H](O)C1)NCC3=CC=C(C4=C(C)N=CS4)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 83.3 mg/mL (159.08 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9097 mL	9.5484 mL	19.0967 mL
5 mM	0.3819 mL	1.9097 mL	3.8193 mL
10 mM	0.1910 mL	0.9548 mL	1.9097 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.78%

Select Batch:

Data Sheet (276 KB) SDS (396 KB)

COA (249 KB) LCMS (136 KB)

Handling Instructions (2659 KB)

References

[1]. Frost J, et al. Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. Nat Commun. 2016 Nov 4;7:13312. [Content Brief]

Kinase Assay ^[1]	VH-298 is screened at 50 μM concentration against a panel of 50 kinases. The remaining kinase activity is recorded in the end of the assay. The data is reported as average % activity remaining of assay duplicates for each kinase tested^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Death of CTLs is analyzed by staining with 4′,6-diamidino-2-phenylindole (DAPI). Cells are plated in 96-well plates at 1×10⁶ and treated with VHL inhibitors (VH-298) and respective non-binding cis-analogues for 24 h. Cells are spun down and resuspended in HBSS containing DAPI to identify dead and dying populations^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Frost J, et al. Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. Nat Commun. 2016 Nov 4;7:13312. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9097 mL	9.5484 mL	19.0967 mL	47.7418 mL
	5 mM	0.3819 mL	1.9097 mL	3.8193 mL	9.5484 mL
	10 mM	0.1910 mL	0.9548 mL	1.9097 mL	4.7742 mL
	15 mM	0.1273 mL	0.6366 mL	1.2731 mL	3.1828 mL
	20 mM	0.0955 mL	0.4774 mL	0.9548 mL	2.3871 mL
	25 mM	0.0764 mL	0.3819 mL	0.7639 mL	1.9097 mL
	30 mM	0.0637 mL	0.3183 mL	0.6366 mL	1.5914 mL
	40 mM	0.0477 mL	0.2387 mL	0.4774 mL	1.1935 mL
	50 mM	0.0382 mL	0.1910 mL	0.3819 mL	0.9548 mL
	60 mM	0.0318 mL	0.1591 mL	0.3183 mL	0.7957 mL
	80 mM	0.0239 mL	0.1194 mL	0.2387 mL	0.5968 mL
	100 mM	0.0191 mL	0.0955 mL	0.1910 mL	0.4774 mL

VH-298 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VH-2982097381-85-4VH298VH 298Ligands for E3 LigaseHIF/HIF Prolyl-HydroxylaseE3 ligase-recruiting MoietyHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

VH-298

Customer Review

Other Forms of VH-298:

VH-298 Related Antibodies

17 Publications Citing Use of MCE VH-298

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Ligands for E3 Ligase Isoform Specific Products:

View All HIF/HIF Prolyl-Hydroxylase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

VH-298 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

VH-298 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report