2. PROTAC Metabolic Enzyme/Protease Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain E1/E2/E3 Enzyme Apoptosis
  4. PROTAC RNF4 degrader-1

PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader (Kd = 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.

PROTAC RNF4 degrader-1

PROTAC RNF4 degrader-1 Chemical Structure

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PROTAC RNF4 degrader-1 Related Antibodies

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Description

PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader (Kd = 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)

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 Kd 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.

PROTAC RNF4 degrader-1 Related Antibodies

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.
Molecular Weight

866.46

Formula

C47H52ClN5O7S
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC RNF4 degrader-1 Related Classifications

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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:

PROTAC RNF4 degrader-1PROTACsEpigenetic Reader DomainE1/E2/E3 EnzymeApoptosisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseubiquitin-proteasome systemcancer cellsmouse modelDNA damageHepG2 human hepatocellular carcinoma cellsapoptosishepatocellular carcinomaHuh7 human hepatocellular carcinoma cellsBRCA1RNF4Inhibitorinhibitorinhibit

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