1. PROTAC
  2. Ligand for E3 Ligase
  3. VH-298

VH-298 

Cat. No.: HY-100947 Purity: 99.32%
Handling Instructions

VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM, used in PROTAC technology.

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

VH-298 Chemical Structure

VH-298 Chemical Structure

CAS No. : 2097381-85-4

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10 mM * 1 mL in DMSO USD 161 In-stock
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10 mg USD 240 In-stock
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50 mg USD 750 In-stock
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100 mg USD 1200 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM, used in PROTAC technology.

IC50 & Target

Kd: 80 to 90 nM (VHL:HIF-α)[1]

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 Kd 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].

Molecular Weight

523.65

Formula

C₂₇H₃₃N₅O₄S

CAS No.

2097381-85-4

SMILES

O=C([[email protected]]1N(C([[email protected]](C(C)(C)C)NC(C2(CC2)C#N)=O)=O)C[[email protected]](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)

*"≥" 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.77 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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

Purity: 99.32%

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Keywords:

VH-298VH298VH 298Ligand for E3 LigaseE3 ligase-recruiting MoietyInhibitorinhibitorinhibit

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VH-298
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