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PROTAC IRAK4 degrader-14
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Catalog No. T217972 Copy Product Info
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PROTAC IRAK4 degrader-14 is an orally active IRAK4 PROTAC degrader with a DC50 of 2.4 nM. It suppresses pro-inflammatory responses in various cell types, including T cells, monocytes, and keratinocytes. PROTAC IRAK4 degrader-14 is applicable in psoriasis-related research.
PROTAC IRAK4 degrader-14
Cas No. 3113890-51-7
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Chemical Properties
Storage & Solubility Information
| Description | PROTAC IRAK4 degrader-14 is an orally active IRAK4 PROTAC degrader with a DC50 of 2.4 nM. It suppresses pro-inflammatory responses in various cell types, including T cells, monocytes, and keratinocytes. PROTAC IRAK4 degrader-14 is applicable in psoriasis-related research. |
| Targets & IC50 | IRAK4:2.4 nM (DC50) |
| In vitro | PROTAC IRAK4 degrader-14 (Compound Ori-Zim-6), at 250 nM for 3-24 hours, induces time-dependent degradation of IRAK4 in the human monocytic cell line THP-1, achieving over 90% degradation within 12 hours and complete degradation by 24 hours. At concentrations of 250-500 nM over 12-24 hours, it promotes proteasome, NCL, and MDM2-dependent ubiquitination and degradation of IRAK4, facilitating the assembly of the MDM2-NCL-PROTAC-IRAK4 quaternary complex. PROTAC IRAK4 degrader-14 also concentration-dependently inhibits LPS-induced mRNA expression of pro-inflammatory mediators (CCL2, CXCL8, IL-6, TNF-α) in human monocytic THP-1 cells when used at 0.01-1 μM for 24 hours. Additionally, it reduces mRNA expression of pro-inflammatory cytokines (TNF-α, IL-2, IFN-γ) in human Jurkat T cells, and inhibits IL-1β-induced pro-inflammatory mediators (TNF-α, IL-6, CXCL8, IL-19) in HaCaT keratinocytes, all in a concentration-dependent manner at 0.01-1 μM for 24 hours. |
| In vivo | PROTAC IRAK4 degrader-14 (Compound Ori-Zim-6) administered at 20 mg/kg orally once daily for 5 days demonstrated significant efficacy in an Imiquimod (IMQ)-induced psoriasis mouse model. The compound also exhibited favorable safety profiles, including recovery of body weight and normalization of serum liver function indicators. |
| Molecular Weight | 1074.20 |
| Formula | C59H68FN5O13 |
| Cas No. | 3113890-51-7 |
| Smiles | O[C@]12[C@]34[C@]([C@]5([C@]([C@@H]1O)([C@@](C)(C)CC[C@H]5O)[H])CO2)(CC[C@]([C@H]3OC(CCC(=O)N6CC7(CC6)CCN(C(=O)C8=CC=C(C#CC=9C%10=C(C(OC[C@H]%11[C@@H](CC)[C@@H](F)C(=O)N%11)=NC9)C=C(OC)C(C(N)=O)=C%10)C=C8)CC7)=O)(C(=C)C4=O)[H])[H] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Related Tags: PROTAC IRAK4 degrader-14 in vivo | PROTAC IRAK4 degrader-14 in vitro | PROTAC IRAK4 degrader-14 formula | PROTAC IRAK4 degrader-14 molecular weight
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