Cat. No.: HY-181692

PROTAC RNF4 degrader-1

Name: PROTAC RNF4 degrader-1
Brand: MedChemExpress
SKU: HY-181692
Price: 850.00 USD
Availability: InStock
Rating: 5 (1 reviews)

Customer Review

Based on 1 Customer Validation

PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader (K_d= 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system. PROTAC RNF4 degrader-1 induces DNA damage, apoptosis, and exhibits antiproliferative activity in cancer cells. PROTAC RNF4 degrader-1 displays antitumor activity with no obvious side effects in mouse models. PROTAC RNF4 degrader-1 is applicable to the research of hepatocellular carcinoma.
(Pink: RNF4 ligand (HY-143346); Blue: VHL ligand (HY-125845); Black: linker).

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

Purity: 98.09%
Formula: C₄₇H₅₂ClN₅O₇S
Molecular Weight:866.46

Storage:

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

PROTAC RNF4 degrader-1 Chemical Structure

Size

Price

Stock

Quantity

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader (K_d= 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system. PROTAC RNF4 degrader-1 induces DNA damage, apoptosis, and exhibits antiproliferative activity in cancer cells. PROTAC RNF4 degrader-1 displays antitumor activity with no obvious side effects in mouse models. PROTAC RNF4 degrader-1 is applicable to the research of hepatocellular carcinoma^[1]. (Pink: RNF4 ligand (HY-143346); Blue: VHL ligand (HY-125845); Black: linker).

IC₅₀ & Target

^[1]

VHL	RNF4 64.5 nM (Kd)

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

In Vitro

PROTAC RNF4 degrader-1 (Compound RD12) (0.2-20 μM; 72 h) potently inhibits the proliferation of HepG2 human hepatocellular carcinoma cells with an IC₅₀ of 0.48 μM^[1].
PROTAC RNF4 degrader-1 (0.1-10 μM; 6 h) induces dose-dependent degradation of RNF4 protein in HepG2 human hepatocellular carcinoma cells^[1].
PROTAC RNF4 degrader-1 (0-20 μM; 6 h) induces dose-dependent degradation of RNF4 protein in Huh7 human hepatocellular carcinoma cells with a DC₅₀ of 4.16 μM^[1].
PROTAC RNF4 degrader-1 (5 μM; 6 h after 2 h pre-incubation with MG132)-mediated RNF4 degradation in HepG2 and Huh7 human hepatocellular carcinoma cells is dependent on the ubiquitin-proteasome system, as pre-treatment with proteasome inhibitor MG132 reverses RNF4 loss^[1].
PROTAC RNF4 degrader-1 (0.1-10 μM; 6 h) induces dose-dependent DNA damage in HepG2 and Huh7 human hepatocellular carcinoma cells, as measured by increased γH2AX levels^[1].
PROTAC RNF4 degrader-1 (0-20 μM; 6 h) increases levels of RNF4 substrate proteins BRCA1 and MDC1 in a dose-dependent manner in Huh7 human hepatocellular carcinoma cells, consistent with RNF4 degradation^[1].
PROTAC RNF4 degrader-1 (serial two-fold dilutions; 30 min at room temperature) binds directly to recombinant RNF4 protein with a K_d of 64.5 nM, as measured by MST^[1].
PROTAC RNF4 degrader-1 (10 μM; 6 h) selectively induces degradation of RNF4 in Huh7 human hepatocellular carcinoma cells, with only 28 of 7483 identified proteins showing significant down-regulation^[1].
PROTAC RNF4 degrader-1 (5 μM; 48 h) induces apoptosis in 52.1% of Huh7 human hepatocellular carcinoma cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

HepG2 human hepatocellular carcinoma cells
Concentration:

0.2, 2, 20 μM
Incubation Time:

72 h
Result:

Inhibited HepG2 cell proliferation with an IC₅₀ of 0.48 ± 0.095 μM.

Western Blot Analysis^[1]

Cell Line:

HepG2 human hepatocellular carcinoma cells
Concentration:

0.1, 1.25, 2.5, 5, 10 μM
Incubation Time:

6 h
Result:

Induced dose-dependent degradation of RNF4 protein, with reduced RNF4 levels observed at all tested concentrations relative to untreated cells.

Western Blot Analysis^[1]

Cell Line:

Huh7 human hepatocellular carcinoma cells
Concentration:

0.1, 1.25, 2.5, 5, 10 μM; 0, 0.625, 1.25, 2.5, 5, 10, 20 μM
Incubation Time:

6 h
Result:

Induced dose-dependent degradation of RNF4 protein with a DC₅₀ (degradation half-maximal concentration) of 4.16 ± 0.222 μM.

Western Blot Analysis^[1]

Cell Line:

HepG2 and Huh7 human hepatocellular carcinoma cells
Concentration:

5 μM
Incubation Time:

6 h (after 2 h pre-incubation with MG132)
Result:

Mediated RNF4 degradation that was rescued by pre-treatment with MG132, confirming dependency on the ubiquitin-proteasome system.

Western Blot Analysis^[1]

Cell Line:

HepG2 and Huh7 human hepatocellular carcinoma cells
Concentration:

0.1, 1.25, 2.5, 5, 10 μM
Incubation Time:

6 h
Result:

Induced dose-dependent increases in γH2AX levels (a marker of DNA double-strand breaks), with higher γH2AX expression observed at higher concentrations.

Western Blot Analysis^[1]

Cell Line:

Huh7 human hepatocellular carcinoma cells
Concentration:

0, 5, 10, 20 μM
Incubation Time:

6 h
Result:

Induced dose-dependent increases in BRCA1 and MDC1 protein levels (known substrates of RNF4), corresponding to reduced RNF4 levels.

Apoptosis Analysis^[1]

Cell Line:

Huh7 human hepatocellular carcinoma cells
Concentration:

5 μM
Incubation Time:

48 h
Result:

Induced apoptosis in 52.1% of Huh7 cells, as measured by Annexin V staining.

In Vivo

PROTAC RNF4 degrader-1 (Compound RD12) (5-20 mg/kg; i.p.; once every two days; 20 days) induces significant dose-dependent hepatocellular carcinoma tumor growth inhibition in BALB/c nude mice, with 58% and 76% inhibition at 5 mg/kg and 20 mg/kg respectively, without causing observable liver toxicity or body weight loss^[1].

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

Animal Model:

BALB/c nude (6-week-old, female, subcutaneously implanted with Huh7 cells)^[1]
Dosage:

5 mg/kg; 20 mg/kg
Administration:

i.p.; once every two days; 20 days
Result:

Achieved tumor growth inhibition rates of 58% at 5 mg/kg and 76% at 20 mg/kg compared to vehicle controls.
Induced significant degradation of RNF4 protein in tumor tissues at 5 mg/kg.
Caused no significant changes in mouse body weight.
Resulted in serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels similar to healthy controls, indicating no liver toxicity.

Chemical Information

Appearance Solid
Molecular Weight 866.46
Formula C₄₇H₅₂ClN₅O₇S
Color White to off-white
SMILES

ClCC(N(CC1=CC=CC=C1)C(C=C2)=CC=C2OC(C=C3)=CC=C3OCCCC(N[C@H](C(N4C[C@@H](C[C@H]4C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)O)=O)C(C)(C)C)=O)=O
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 : 200 mg/mL (230.82 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

1.1541 mL

5.7706 mL

11.5412 mL

5 mM

0.2308 mL

1.1541 mL

2.3082 mL

10 mM

0.1154 mL

0.5771 mL

1.1541 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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: ≥ 5 mg/mL (5.77 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (5.77 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)

References

[1]. Wan H, et al. Development of the first-in-class RNF4 PROTAC degrader as potential therapeutics for hepatocellular carcinoma. Eur J Med Chem. 2026;307:118668. [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	1.1541 mL	5.7706 mL	11.5412 mL	28.8530 mL
	5 mM	0.2308 mL	1.1541 mL	2.3082 mL	5.7706 mL
	10 mM	0.1154 mL	0.5771 mL	1.1541 mL	2.8853 mL
	15 mM	0.0769 mL	0.3847 mL	0.7694 mL	1.9235 mL
	20 mM	0.0577 mL	0.2885 mL	0.5771 mL	1.4427 mL
	25 mM	0.0462 mL	0.2308 mL	0.4616 mL	1.1541 mL
	30 mM	0.0385 mL	0.1924 mL	0.3847 mL	0.9618 mL
	40 mM	0.0289 mL	0.1443 mL	0.2885 mL	0.7213 mL
	50 mM	0.0231 mL	0.1154 mL	0.2308 mL	0.5771 mL
	60 mM	0.0192 mL	0.0962 mL	0.1924 mL	0.4809 mL
	80 mM	0.0144 mL	0.0721 mL	0.1443 mL	0.3607 mL
	100 mM	0.0115 mL	0.0577 mL	0.1154 mL	0.2885 mL

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PROTAC RNF4 degrader-1

All PROTACs Isoforms

All Epigenetic Reader Domain Isoforms