2. PROTAC
  3. Molecular Glues
  4. NVS-VHL720

NVS-VHL720 is a selective VHL-based cysteine dioxygenase (CDO1) molecular glue degrader. NVS-VHL720 recruits CDO1 to the VHL E3 ligase complex, driving ubiquitin-dependent proteasomal degradation of CDO1. NVS-VHL720 can be used for the research of cancer.

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NVS-VHL720

NVS-VHL720 構造式

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 649 在庫あり
Solution
10 mM * 1 mL in DMSO USD 649 在庫あり
Solid
5 mg $600 在庫あり
10 mg $950 在庫あり
25 mg $1820 在庫あり
50 mg $2900 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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NVS-VHL720 関連抗体

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  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

NVS-VHL720 is a selective VHL-based cysteine dioxygenase (CDO1) molecular glue degrader. NVS-VHL720 recruits CDO1 to the VHL E3 ligase complex, driving ubiquitin-dependent proteasomal degradation of CDO1. NVS-VHL720 can be used for the research of cancer[1].

IC50 & Target

Cysteine dioxygenase (CDO1)[1]
体外実験

NVS-VHL720 (Compound 8) binds directly to VHL with a Kd of 0.072 μM, and mediates formation of a high-affinity ternary VBC-CDO1 complex with a Kd of 0.10 μM, which is drastically reduced by mutation of CDO1 residue Q99[1].
NVS-VHL720 (60 min) potently induces ternary VBC-CDO1 complex formation in a TR-FRET assay with an AC50 of 0.071 μM, and this activity is significantly reduced by mutation of CDO1 residue Q99[1].
NVS-VHL720 (2 h) induces VHL-CDO1 ternary complex formation in HEK293T cells with an AC50 of 0.306 μM, as measured by the NanoBiT assay[1].
NVS-VHL720 (17 h) potently degrades CDO1 in HEK293T cells with an absDC50 of 0.008 μM and 98.46% maximum degradation, and this activity is dependent on CDO1 residue Q99[1].
NVS-VHL720 (0.05-0.1 μM; 24 h) selectively degrades endogenous CDO1 in Huh-7 cells, with 62% degradation at 0.05 μM and 72% degradation at 0.1 μM, without affecting other quantified proteins[1].
NVS-VHL720 (0.01 nM-100 μM) does not affect the viability of HEK293T cells at tested concentrations[1].

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

NVS-VHL720 関連抗体
分子量

491.58

分子式

C27H33N5O4
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC1=CC=C(C2=CC=NN2)C3=C1C=CC=C3)[C@H]4N(C([C@@H](NC(C)=O)C(C)(C)C)=O)C[C@H](O)C4
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (203.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0343 mL 10.1713 mL 20.3426 mL
5 mM 0.4069 mL 2.0343 mL 4.0685 mL
10 mM 0.2034 mL 1.0171 mL 2.0343 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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: ≥ 5 mg/mL (10.17 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (10.17 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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.
純度とドキュメンテーション
参考文献

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0343 mL 10.1713 mL 20.3426 mL 50.8564 mL
5 mM 0.4069 mL 2.0343 mL 4.0685 mL 10.1713 mL
10 mM 0.2034 mL 1.0171 mL 2.0343 mL 5.0856 mL
15 mM 0.1356 mL 0.6781 mL 1.3562 mL 3.3904 mL
20 mM 0.1017 mL 0.5086 mL 1.0171 mL 2.5428 mL
25 mM 0.0814 mL 0.4069 mL 0.8137 mL 2.0343 mL
30 mM 0.0678 mL 0.3390 mL 0.6781 mL 1.6952 mL
40 mM 0.0509 mL 0.2543 mL 0.5086 mL 1.2714 mL
50 mM 0.0407 mL 0.2034 mL 0.4069 mL 1.0171 mL
60 mM 0.0339 mL 0.1695 mL 0.3390 mL 0.8476 mL
80 mM 0.0254 mL 0.1271 mL 0.2543 mL 0.6357 mL
100 mM 0.0203 mL 0.1017 mL 0.2034 mL 0.5086 mL
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NVS-VHL720 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

NVS-VHL720Molecular GluesX-ray structureCDO1VHL E3 ligase complexubiquitinmammalian cellsHuh-7 cellscullin-ring ligase complexVBC-CDO1 complexproteasomal degradationHEK293T cellsInhibitorinhibitorinhibit

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製品名:
NVS-VHL720
製品番号:
HY-160525
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