PROTAC NCOA4 degrader-1
Based on 1 Customer Validation
PROTAC NCOA4 degrader-1 is a VHL-based PROTAC NCOA4 degrader. PROTAC NCOA4 degrader-1 is a ferroptosis inhibitor. PROTAC NCOA4 degrader-1 reduces Fe2+ elevation, ROS production, MDA content and PTGS2 mRNA expression. PROTAC NCOA4 degrader-1 ameliorates liver damage in a CCl4-induced acute liver injury model. PROTAC NCOA4 degrader-1 can be used for the researches of inflammation and immunology.
For research use only. We do not sell to patients.
- Purity : 99.75%
- CAS No.: 3098187-24-4
- Formula: C62H80N10O9S
- Molecular Weight:1141.43
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
VHL |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AML12 | EC50 |
0.009 μM
Compound: V3
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Protection against CCl4-induced ferroptosis in mouse AML12 cells assessed as cell viability in presence of Ferrostatin-1
Protection against CCl4-induced ferroptosis in mouse AML12 cells assessed as cell viability in presence of Ferrostatin-1
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[PMID: 39047113] |
| AML12 | EC50 |
0.41 μM
Compound: V3
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Protection against CCl4-induced ferroptosis in mouse AML12 cells assessed as cell viability in presence of Deferoxamine
Protection against CCl4-induced ferroptosis in mouse AML12 cells assessed as cell viability in presence of Deferoxamine
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[PMID: 39047113] |
In Vitro
PROTAC NCOA4 degrader-1 (Compound V3) (3-24 h) induces NCOA4 degradation via the ubiquitin-proteasome system (UPS) in HeLa cells, with a DC50 of 3 nM[1].
PROTAC NCOA4 degrader-1 (24 h) degrades NCOA4 in AML12 murine hepatocytes with a DC50 of 202 nM and does not affectNCOA4 mRNA level[1].
PROTAC NCOA4 degrader-1 (0.04-10 μM, 24 h) upregulates the protein levels of ferritin heavy chain (FTH1) and light chain (FTL) in AML12 cells[1].
PROTAC NCOA4 degrader-1 (200 nM, 36 h) reduces intracellular free Fe2+ level and lipid hydroperoxide level in AML12 cells[1].
PROTAC NCOA4 degrader-1 (200 nM, 48 h) inhibits ferroptosis and restores cell viability in AML12 cells[1].
PROTAC NCOA4 degrader-1 (0.2-1 μM, 36 h) reduces CCl4-induced Fe2+ elevation, ROS production, MDA content, and PTGS2 mRNA expression in AML12 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:AML12 cells
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Concentration:0.04, 0.12, 0.36, 1.1, 3.3 and 10 μM
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Incubation Time:24 h
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Result:Reduced the levels of ferritin heavy chain (FTH1) and light chain (FTL).
Showed no significant effect on FTH1/FTL mRNA.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CCl4-induced acute liver injury C57BL/6 mice models[1]
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Dosage:10 and 30 mg/kg
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Administration:Intraperitoneally injection, 3 h before CCl4
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Result:Degraded NCOA4 in mouse liver tissue.
Upregulated FTH1/FTL levels.
Reduced hepatic iron deposition.
Decreased hepatic MDA content and PTGS2 mRNA expression.
Reduced serum ALT/AST levels and decreased TUNEL-positive cells.
Downregulated the levels of inflammatory factors IL-1β, IL-6, and TNF-α in serum and liver tissue.
Chemical Information
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CAS No. 3098187-24-4
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Appearance Solid
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Molecular Weight 1141.43
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Formula C62H80N10O9S
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Color White to off-white
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SMILES
CN1CCN(C2=CC3=C(N=C(C4=CC(N5CCC6=CC(OCCOCCOCCOCCNC(CCCC(N[C@H](C(C)(C)C)C(N7[C@@H](C[C@H](C7)O)C(NCC8=CC=C(C=C8)C9=C(N=CS9)C)=O)=O)=O)=O)=CC=C6C5)=CC=C4)N3)C=C2)CC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (87.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.19 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.19 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 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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RT-PCR
Reverse transcription technology uses RNA as a template to synthesize DNA. RT-PCR is simple, specific and sensitive, and can be used to detect gene expression levels and expression differences in cells; detect RNA virus content; clone cDNA sequences of specific genes.
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Ferroptosis Solutions
Ferroptosis is an iron-dependent, non-apoptotic form of regulated cell death characterized by lethal lipid peroxidation and sensitivity to suppression by iron chelators or lipophilic radical-trapping antioxidants. The core pathway links cystine uptake through system Xc−, glutathione availability, GPX4-dependent detoxification of phospholipid hydroperoxides, iron-dependent oxidative reactions, and polyunsaturated-phospholipid metabolism into a cell-death program that is biochemically and morphologically distinct from apoptosis, necrosis, and autophagy. The ferroptosis pathway is experimentally linked to phenotype through chemical and genetic perturbation. Erastin induces ferroptosis by inhibiting cystine uptake through system Xc− and weakening antioxidant defenses, while GPX4 inhibition or depletion causes lipid peroxide accumulation and ferroptotic cancer-cell death. ACSL4 and oxidizable arachidonoyl- or adrenoyl-containing phosphatidylethanolamines shape ferroptosis sensitivity by con
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Hepatotoxicity Study
This protocol evaluates hepatotoxicity using complementary in vivo mouse APAP acute liver injury and in vitro hepatocyte-based cytotoxicity readouts. In vivo APAP injury is assessed by serum ALT/AST, liver histology, hepatic glutathione, protein adducts, necrosis, inflammation, and regeneration-related endpoints. In vitro hepatotoxicity is assessed by loss of viability, leakage of ALT/AST/LDH, oxidative-stress markers, mitochondrial function, nuclear morphology, intracellular calcium, and high-content imaging endpoints.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Real Time qPCR (Q-PCR)
Real-time quantitative PCR (qPCR) quantifies an amplifiable nucleic-acid target by monitoring fluorescence during PCR cycling rather than measuring product only after amplification. The increase in fluorescence tracks accumulation of PCR product, and the quantification cycle (Cq; historically also Ct/CP) is related to the initial amount of target: samples containing more starting target generally reach the defined fluorescence threshold in fewer cycles.
Purity & Documentation
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Data Sheet (271 KB)
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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)
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Handling Instructions (2659 KB)
References
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 (protect from light, stored under nitrogen). 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 | 0.8761 mL | 4.3805 mL | 8.7609 mL | 21.9023 mL |
| 5 mM | 0.1752 mL | 0.8761 mL | 1.7522 mL | 4.3805 mL | |
| 10 mM | 0.0876 mL | 0.4380 mL | 0.8761 mL | 2.1902 mL | |
| 15 mM | 0.0584 mL | 0.2920 mL | 0.5841 mL | 1.4602 mL | |
| 20 mM | 0.0438 mL | 0.2190 mL | 0.4380 mL | 1.0951 mL | |
| 25 mM | 0.0350 mL | 0.1752 mL | 0.3504 mL | 0.8761 mL | |
| 30 mM | 0.0292 mL | 0.1460 mL | 0.2920 mL | 0.7301 mL | |
| 40 mM | 0.0219 mL | 0.1095 mL | 0.2190 mL | 0.5476 mL | |
| 50 mM | 0.0175 mL | 0.0876 mL | 0.1752 mL | 0.4380 mL | |
| 60 mM | 0.0146 mL | 0.0730 mL | 0.1460 mL | 0.3650 mL | |
| 80 mM | 0.0110 mL | 0.0548 mL | 0.1095 mL | 0.2738 mL |
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