dIRF4-2
Based on 1 Customer Validation
dIRF4-2 is a selective IRF4 PROTAC degrader with a DC50 value of 2.2 μM. dIRF4-2 forms a ternary complex between IRF4 and CRBN, inducing ubiquitination and proteasomal degradation of IRF4. dIRF4-2 downregulates MYC. dIRF4-2 exhibits anticancer activity against myeloma. dIRF4-2 acts as a chemical probe for investigating IRF4 function, mimicking the IRF4 gene knockout phenotype. dIRF4-2 can be used in the research of multiple myeloma.
(Pink: IRF4 ligand (HY-185698); Blue: Cereblon ligand (HY-14658); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.11%
- CAS No.: 3136609-62-3
- Formula: C43H46N8O7
- Molecular Weight:786.87
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
In Vitro
dIRF4-2 (1-20 μM; 24 h) induces dose-dependent proteasomal degradation of IRF4 in MM1.S and OPM2 multiple myeloma cell lines, with DC50 values of 2.2 μM and 2.3 μM respectively after 24 h of treatment[1].
dIRF4-2 (2.5 μM; 2-10 h) induces rapid and sustained degradation of IRF4 (initiated within 2 h), and treatment with 2.5 μM for up to 10 h does not affect the off-target novel substrate IKZF3 in MM1.S and OPM2 multiple myeloma cell lines[1].
dIRF4-2 (2.5 μM; 2 h) induces the degradation of IRF4 in MM1.S multiple myeloma cells, and this degradation process is proteasome-dependent; co-treatment with 1 μM bortezomib or 1 μM MG132 followed by a 2-hour incubation restores IRF4 levels[1].
dIRF4-2 (2.5 μM; 4 h) induces highly selective degradation of IRF4 in MM1.S multiple myeloma cells, and exerts no significant effects on other IRF family members or novel CRBN substrates after 4 h of treatment at 2.5 μM[1].
dIRF4-2 (100 μM three-fold dilution series; 96 h, with second dose at 48 h) induces potent, IRF4-dependent cytotoxicity in all tested multiple myeloma cell lines after 96 h of treatment (IC50 0.68-8 μM), while exerting no effect on IRF4-independent HEK293T cells (IC50 > 50 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM1.S, OPM2
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Concentration:1, 2.5, 5, 10, 20 μM
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Incubation Time:24 h
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Result:Induced dose-dependent degradation of IRF4 in both MM1.S and OPM2 cell lines.
Reached half-maximal degradation concentration (DC50) of 2.2 μM for MM1.S and 2.3 μM for OPM2.
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Cell Line:MM1.S, OPM2
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Concentration:2.5 μM
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Incubation Time:2, 4, 6, 8, 10 h
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Result:Induced rapid depletion of IRF4 within 2 hours, with sustained degradation through 10 hours.
Showed no degradation of the off-target neosubstrate IKZF3 at any timepoint.
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Cell Line:12 human multiple myeloma cell lines, HEK293T
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Concentration:100 μM three-fold dilution series
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Incubation Time:96 h (with second dose at 48 h)
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Result:Exhibited IRF4-dependent cytotoxicity across all multiple myeloma cell lines tested, with IC50 values ranging from 0.68 μM (Karpas-707) to 8 μM (MOLP-2).
Showed no cytotoxicity in non-IRF4-dependent HEK293T cell line, with an IC50 > 50 μM.
Chemical Information
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CAS No. 3136609-62-3
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Appearance Solid
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Molecular Weight 786.87
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Formula C43H46N8O7
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Color Light yellow to yellow
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SMILES
COC1=CC=C(C2(CC2)C(N[C@H](C(NC)=O)C3=CC=CC(C4=CN(CCCN5CCN(C6=CC=C(C(N(C7C(NC(CC7)=O)=O)C8=O)=O)C8=C6)CC5)N=C4)=C3)=O)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (127.09 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (3.18 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.
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 (sealed storage, away from moisture)
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.
Purity & Documentation
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Data Sheet (273 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 (sealed storage, away from moisture). 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 | 1.2709 mL | 6.3543 mL | 12.7086 mL | 31.7714 mL |
| 5 mM | 0.2542 mL | 1.2709 mL | 2.5417 mL | 6.3543 mL | |
| 10 mM | 0.1271 mL | 0.6354 mL | 1.2709 mL | 3.1771 mL | |
| 15 mM | 0.0847 mL | 0.4236 mL | 0.8472 mL | 2.1181 mL | |
| 20 mM | 0.0635 mL | 0.3177 mL | 0.6354 mL | 1.5886 mL | |
| 25 mM | 0.0508 mL | 0.2542 mL | 0.5083 mL | 1.2709 mL | |
| 30 mM | 0.0424 mL | 0.2118 mL | 0.4236 mL | 1.0590 mL | |
| 40 mM | 0.0318 mL | 0.1589 mL | 0.3177 mL | 0.7943 mL | |
| 50 mM | 0.0254 mL | 0.1271 mL | 0.2542 mL | 0.6354 mL | |
| 60 mM | 0.0212 mL | 0.1059 mL | 0.2118 mL | 0.5295 mL | |
| 80 mM | 0.0159 mL | 0.0794 mL | 0.1589 mL | 0.3971 mL | |
| 100 mM | 0.0127 mL | 0.0635 mL | 0.1271 mL | 0.3177 mL |
dIRF4-2 Related Classifications
HY-185697 Related Classifications
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