Cat. No.: HY-100947

VH-298

17 Cited Publications

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Based on 17 publication(s) in Google Scholar

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.

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Pureté: 99.54%
CAS No.: 2097381-85-4
Formule: C₂₇H₃₃N₅O₄S
Masse moléculaire:523.65

Stockage:

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

VH-298 Chemical Structure

CAS No.: 2097381-85-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (17)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

VHL

Voir tous les produits spécifiques à Isoform Ligands for E3 Ligase :

Voir tous les produits spécifiques à Isoform HIF/HIF Prolyl-Hydroxylase :

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]
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]
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]

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.

Chemical Information

CAS No. 2097381-85-4
Appearance Solid
Masse moléculaire 523.65
Formule C₂₇H₃₃N₅O₄S
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (17)

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Journal Impact Factor

Cancer Cell

A pan-KRAS inhibitor and its derived degrader elicit multifaceted anti-tumor efficacy in KRAS-driven cancers. [Abstract]

2025 Jul 25:S1535-6108(25)00310-1. PMID: 40780213
ACS Nano

Fluorinated Proteolysis Targeting Chimeras-Sorafenib Nanoassembly for Epigenetic Remodeling to Combat Multi-Pathway Drug Resistance in Hepatocellular Carcinoma. [Abstract]

2025 Oct 7;19(39):34659-34676. PMID: 40977536
Nat Chem Biol

Ubiquitin-specific proximity labeling for the identification of E3 ligase substrates. [Abstract]

2024 Sep;20(9):1227-1236. PMID: 38514884
Cell Discov

A PROTAC peptide induces durable β-catenin degradation and suppresses Wnt-dependent intestinal cancer. [Abstract]

2020 Jun 9;6:35. PMID: 32550000
J Control Release

An mRNA vaccine encoding proteasome-targeted antigen enhances CD8+ T cell immunity. [Abstract]

2025 May 10:381:113578. PMID: 40015339
Cell Death Dis

VHL regulates the sensitivity of clear cell renal cell carcinoma to SIRT4-mediated metabolic stress via HIF-1α/HO-1 pathway. [Abstract]

2021 Jun 16;12(7):621. PMID: 34135317

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.
Proc Natl Acad Sci U S A

Dynamic investigation of hypoxia-induced L-lactylation. [Abstract]

2025 Mar 11;122(10):e2404899122. PMID: 40030031
Acta Pharmacol Sin

Inhibiting von Hippel‒Lindau protein-mediated Dishevelled ubiquitination protects against experimental parkinsonism. [Abstract]

2023 May;44(5):940-953. PMID: 36357669

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.
Chem Sci

Unveiling BCL-xL-specific PROTAC efficiency and dissociation pathways using native mass spectrometry. [Abstract]

2026 Feb 19. PMID: 41727719
Cell Chem Biol

PIM1 targeted degradation prevents the emergence of chemoresistance in prostate cancer. [Abstract]

2024 Feb 15;31(2):326-337.e11. PMID: 38016478
Curr Opin Chem Biol

19 October 2021, 100009.
Hepatol Commun

Proteomics-based identification of the role of osteosarcoma amplified-9 in hepatocellular carcinoma recurrence. [Abstract]

2022 Aug;6(8):2182-2197. PMID: 35429130
ACS Omega

Development of BODIPY FL VH032 as a High-Affinity and Selective von Hippel-Lindau E3 Ligase Fluorescent Probe and Its Application in a Time-Resolved Fluorescence Resonance Energy-Transfer Assay. [Abstract]

2020 Dec 29;6(1):680-695. PMID: 33458521
Drug Dev Res

Proteolysis targeting chimera (PROTAC) for epidermal growth factor receptor enhances anti-tumor immunity in non-small cell lung cancer. [Abstract]

2021 May;82(3):422-429. PMID: 33231319
Bioconjug Chem

Development of BODIPY FL Thalidomide As a High-Affinity Fluorescent Probe for Cereblon in a Time-Resolved Fluorescence Resonance Energy Transfer Assay. [Abstract]

2020 Nov 18;31(11):2564-2575. PMID: 33070611
bioRxiv

2025 Jun 19.
bioRxiv

2024 June 12.

Solvant et solubilité

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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:

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g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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

Please enter your animal formula composition:

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

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).

Working solution concentration: 0.22 mg/mL

Protocole

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].

MedChemExpress (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].

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

VH-298

17 Cited Publications

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VH-298

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Ubiquitination Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

E3 Ligase Ligand Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) VH-298

Voir tous les produits spécifiques à Isoform Ligands for E3 Ligase

Voir tous les produits spécifiques à Isoform HIF/HIF Prolyl-Hydroxylase

Activité biologique

Chemical Information

Publications (17)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

VH-298

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Ubiquitination Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

E3 Ligase Ligand Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) VH-298

Voir tous les produits spécifiques à Isoform Ligands for E3 Ligase

Voir tous les produits spécifiques à Isoform HIF/HIF Prolyl-Hydroxylase

Activité biologique

Chemical Information

Publications (17)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

VH-298 Related Classifications

HY-100947 Related Classifications