PROTAC IRAK4 degrader-8
Based on 1 Customer Validation
PROTAC IRAK4 degrader-8 (Compound 2) is a PROTAC degrader that targets IRAK4 by recruiting cereblon. PROTAC IRAK4 degrader-8 inhibits IRAK4 kinase activity with an IC50 of 15.5 nM. PROTAC IRAK4 degrader-8 suppresses IL-6 production in immune cells. PROTAC IRAK4 degrader-8 can be used in the research of inflammatory diseases, immune diseases and cancers.
(Pink: IRAK4 ligand (HY-145484); Blue: Cereblon ligand (HY-161637); Black: linker (HY-30536)).
For research use only. We do not sell to patients.
- Purity: 99.70%
- CAS No.: 2911615-06-8
- Formula: C43H50ClF2N11O5
- Molecular Weight:874.38
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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IRAK4 |
PROTAC IRAK4 degrader-8 (Compound 2) (0.038-10000 nM; 120 min) inhibits IRAK4 kinase activity in a recombinant IRAK4 kinase HTRF assay, with an IC50 of 15.5 nM[1].
PROTAC IRAK4 degrader-8 (0.03-3000 nM; 24 h) concentration-dependently reduces IRAK4 protein levels and induces IRAK4 degradation in THP-1 cells, with a DC50 of 1.8 nM and a Dmax of 95.8%[1].
PROTAC IRAK4 degrader-8 potently inhibits IL-6 production in human peripheral blood mononuclear cells, with an IC50 of 2.2 nM[1].
PROTAC IRAK4 degrader-8 inhibits IL-6 production in human whole blood with an IC50 of 246 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1
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Concentration:0.03-3000 nM
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Incubation Time:24 h
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Result:Concentration-dependently reduced IRAK4 protein levels.
Chemical Information
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CAS No. 2911615-06-8
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Appearance Solid
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Molecular Weight 874.38
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Formula C43H50ClF2N11O5
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Color White to off-white
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SMILES
O=C(C(C=C1)=CC(N(CCC2=O)C(N2)=O)=C1Cl)N3CCC(CCN4C[C@H]5CC[C@H](N(N=C6C(F)F)C=C6NC(C7=C(N=C(N8[C@](CO9)([H])C[C@]9([H])C8)C=C%10)N%10N=C7)=O)CC5)(CC4)CC3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (114.37 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. 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. 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)
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 (2.86 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 (2.86 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.
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.
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 (270 KB)
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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)
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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. 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 |
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| DMSO | 1 mM | 1.1437 mL | 5.7183 mL | 11.4367 mL | 28.5917 mL |
| 5 mM | 0.2287 mL | 1.1437 mL | 2.2873 mL | 5.7183 mL | |
| 10 mM | 0.1144 mL | 0.5718 mL | 1.1437 mL | 2.8592 mL | |
| 15 mM | 0.0762 mL | 0.3812 mL | 0.7624 mL | 1.9061 mL | |
| 20 mM | 0.0572 mL | 0.2859 mL | 0.5718 mL | 1.4296 mL | |
| 25 mM | 0.0457 mL | 0.2287 mL | 0.4575 mL | 1.1437 mL | |
| 30 mM | 0.0381 mL | 0.1906 mL | 0.3812 mL | 0.9531 mL | |
| 40 mM | 0.0286 mL | 0.1430 mL | 0.2859 mL | 0.7148 mL | |
| 50 mM | 0.0229 mL | 0.1144 mL | 0.2287 mL | 0.5718 mL | |
| 60 mM | 0.0191 mL | 0.0953 mL | 0.1906 mL | 0.4765 mL | |
| 80 mM | 0.0143 mL | 0.0715 mL | 0.1430 mL | 0.3574 mL | |
| 100 mM | 0.0114 mL | 0.0572 mL | 0.1144 mL | 0.2859 mL |
PROTAC IRAK4 degrader-8 Related Classifications
HY-153673 Related Classifications
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