Art. -Nr.: HY-159779

NR-V04

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NR-V04 is a selective NR4A1 PROTAC degrader. NR-V04 forms a ternary complex with NR4A1 and the VHL E3 ligase, mediates proteasome-dependent degradation of NR4A1. NR-V04 induces tumor-infiltrating B cells and effector memory CD8⁺ T cells and reduces monocytic myeloid-derived suppressor cells in tumor microenvironments. NR-V04 can be used for the research of melanoma and colon cancer.
(Pink: Nur77/NR4A1 ligand (HY-13067); Blue: VHL ligand (HY-112078); Black: linker (HY-130524)).

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Reinheit: 99.90%
CAS. Nr.: 2766608-52-8
Formel: C₆₂H₈₇N₅O₁₁S
Molecular Weight:1110.45

Speicherung:

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

NR-V04 Chemical Structure

CAS. Nr.: 2766608-52-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

NR-V04 is a selective NR4A1 PROTAC degrader. NR-V04 forms a ternary complex with NR4A1 and the VHL E3 ligase, mediates proteasome-dependent degradation of NR4A1. NR-V04 induces tumor-infiltrating B cells and effector memory CD8⁺ T cells and reduces monocytic myeloid-derived suppressor cells in tumor microenvironments. NR-V04 can be used for the research of melanoma and colon cancer^[1]. (Pink: Nur77/NR4A1 ligand (HY-13067); Blue: VHL ligand (HY-112078); Black: linker (HY-130524)).

IC₅₀ & Target^[1]

VHL	Nur77/NR4A1

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Nuclear Hormone Receptor 4A/NR4A Isoform-spezifische Produkte anzeigen :

In Vitro

NR-V04 (250 nM; 16 h) potently reduces NR4A1 protein levels in CHL-1 human melanoma cells^[1].
NR-V04 (125-1000 nM; 16 h) induces dose-dependent NR4A1 degradation in CHL-1 (DC₅₀ = 228.5 nM) and A375 (DC₅₀ = 518.8 nM) human melanoma cells without affecting NR4A2 or NR4A3 levels, while accumulating VHL protein^[1].
NR-V04 (500-1000 nM; 16 h) reduces NR4A1 protein levels in WM164, M229 human melanoma cells, and SM1, SW1 mouse melanoma cells^[1].
NR-V04 (500 nM; 4-48 h) induces time-dependent NR4A1 degradation in CHL-1 human melanoma cells, with an initial protein induction at 4 h and efficient degradation occurring between 8 and 48 h^[1].
NR-V04 (500 nM; 16 h) induces ternary complex formation between NR4A1 and VHL in HEK293T cells overexpressing Flag-NR4A1^[1].
NR-V04 (500 nM) significantly reduces the percentage of exhausted CD8⁺ T cells in human PBMC-derived CD8⁺ T cell cultures^[1].

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

Western Blot Analysis^[1]

Cell Line:

CHL-1, A375 human melanoma cells
Concentration:

125, 250, 500, 1000 nM
Incubation Time:

16 h
Result:

Induced a dose-dependent decrease of NR4A1 protein with a DC50 of 228.5 nM in CHL-1 cells and a DC50 of 518.8 nM in A375 cells.
Led to accumulation of VHL protein in both cell lines.
Selectively reduced NR4A1 protein levels.
Spared NR4A2 and NR4A3 protein levels in both cell lines.

Parmacokinetics

Species	Dose	Route	AUC_0-inf	T_1/2	CL	MRT_0-inf	V_ss	T_max	C_max	F
Mice^[1]	2 mg/kg	i.v.	3492 ng·h/mL	5.36 h	9.74 mL/h/kg	1.79 h	1.05 L/kg	/	/	/
Mice^[1]	20 mg/kg	i.p.	34218 ng·h/mL	8.58 h	/	11.7 h	/	1.17 h	3110 ng/mL	98 %

In Vivo

NR-V04 (1.8 mg/kg; i.p.; at day 7) exhibits antitumor effects in several tumor mice models^[1].

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

Animal Model:

C57BL/6J mice with B16F10, MC38 and Yumm1.7 (7-9 weeks)^[1]
Dosage:

1.8 mg/kg
Administration:

I.p.; at day 7
Result:

Inhibited tumor growth.
Increased B cell percentage in the TME, but not in spleen and blood.
Induces tumor-infiltrating B cells and effector memory CD8+ T cells.
Reduced monocytic myeloid-derived suppressor cells in tumor microenvironments.

Chemical Information

CAS. Nr. 2766608-52-8
Appearance Solid
Molecular Weight 1110.45
Formel C₆₂H₈₇N₅O₁₁S
Color Orange to red
SMILES

C[C@@]12[C@]([C@@]3([H])[C@@](CC1)(CC[C@](C)(C3)C(NCCOCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@H](C4)O)C(N[C@H](C5=CC=C(C6=C(N=CS6)C)C=C5)C)=O)=O)=O)=O)C)(CC[C@@]7(C2=CC=C8C7=CC(C(O)=C8C)=O)C)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (90.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

0.9005 mL

4.5027 mL

9.0054 mL

5 mM

0.1801 mL

0.9005 mL

1.8011 mL

10 mM

0.0901 mL

0.4503 mL

0.9005 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 (2.25 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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)
Handling Instructions (2659 KB)

Verweise

[1]. Wang L, et al. PROTAC-mediated NR4A1 degradation as a novel strategy for cancer immunotherapy. J Exp Med. 2024;221(3):e20231519. [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	0.9005 mL	4.5027 mL	9.0054 mL	22.5134 mL
	5 mM	0.1801 mL	0.9005 mL	1.8011 mL	4.5027 mL
	10 mM	0.0901 mL	0.4503 mL	0.9005 mL	2.2513 mL
	15 mM	0.0600 mL	0.3002 mL	0.6004 mL	1.5009 mL
	20 mM	0.0450 mL	0.2251 mL	0.4503 mL	1.1257 mL
	25 mM	0.0360 mL	0.1801 mL	0.3602 mL	0.9005 mL
	30 mM	0.0300 mL	0.1501 mL	0.3002 mL	0.7504 mL
	40 mM	0.0225 mL	0.1126 mL	0.2251 mL	0.5628 mL
	50 mM	0.0180 mL	0.0901 mL	0.1801 mL	0.4503 mL
	60 mM	0.0150 mL	0.0750 mL	0.1501 mL	0.3752 mL
	80 mM	0.0113 mL	0.0563 mL	0.1126 mL	0.2814 mL

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NR-V04

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Transcription Factor-Targeted Library

Anti-Colorectal Cancer Compound Library

Nuclear Receptor Compound Library

PROTAC Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Nuclear Hormone Receptor 4A/NR4A Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NR-V04

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Transcription Factor-Targeted Library

Anti-Colorectal Cancer Compound Library

Nuclear Receptor Compound Library

PROTAC Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Nuclear Hormone Receptor 4A/NR4A Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NR-V04 Related Classifications

Art. -Nr.: HY-159779