PROTAC IRAK4 degrader-13

Cat. No.: HY-175022 Purity: 99.47%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

PROTAC IRAK4 degrader-13 (Degrader 1) is a selective IRAK4 PROTAC degrader with DC₅₀s of 0.86 and 1.1 nM for monocytes and lymphocytes in PBMCs, respectively. PROTAC IRAK4 degrader-13 significantly induces TIR signal activation, and inhibits the expression of circulating proinflammatory cytokines in Imiquimod (HY-B0180) induced psoriasis mice model. PROTAC IRAK4 degrader-13 can be used for TLR- and IL-1R-driven driven neutrophilic inflammation diseases like hidradenitis suppurativa (HS) and atopic dermatitis (AD) research. Pink: IRAK4 ligand; Blue: E3 ligase ligand; Black: linker

For research use only. We do not sell to patients.

PROTAC IRAK4 degrader-13 Chemical Structure

CAS No. : 2432992-21-5

Size	Price	Stock
5 mg		Ask For Quote & Lead Time
10 mg		Ask For Quote & Lead Time
25 mg		Ask For Quote & Lead Time
50 mg		Ask For Quote & Lead Time

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This product is a controlled substance and not for sale in your territory.

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

Biological Activity
Purity & Documentation
References
Customer Review

Description

PROTAC IRAK4 degrader-13 (Degrader 1) is a selective IRAK4 PROTAC degrader with DC₅₀s of 0.86 and 1.1 nM for monocytes and lymphocytes in PBMCs, respectively. PROTAC IRAK4 degrader-13 significantly induces TIR signal activation, and inhibits the expression of circulating proinflammatory cytokines in Imiquimod (HY-B0180) induced psoriasis mice model. PROTAC IRAK4 degrader-13 can be used for TLR- and IL-1R-driven driven neutrophilic inflammation diseases like hidradenitis suppurativa (HS) and atopic dermatitis (AD) research^[1]. Pink: IRAK4 ligand; Blue: E3 ligase ligand; Black: linker

IC₅₀ & Target^[1]

IRAK4

IL-6

IL-8

IL-17

IL-22

IL-23

IL-1b

Molecular Weight

843.94

Formula

C₄₄H₅₂F₃N₉O₅

CAS No.

2432992-21-5

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NC(C(F)(F)F)=CC=C1)NC2=CC3=CN([C@H]4CC[C@H](CN(C5CCN(CC6=C(C(N7C(CC8)C(NC8=O)=O)=CC=C6)N(C)C7=O)CC5)C)CC4)N=C3C=C2C(C)(O)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (118.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.1849 mL	5.9246 mL	11.8492 mL
5 mM	0.2370 mL	1.1849 mL	2.3698 mL
10 mM	0.1185 mL	0.5925 mL	1.1849 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.96 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.96 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.47%

Select Batch:

Data Sheet (269 KB) SDS (252 KB)

COA (245 KB) HNMR (154 KB) RP-HPLC (163 KB) LCMS (108 KB)

Handling Instructions (2659 KB)

References

[1]. Veronica C,et al. Irak degraders and uses thereof. WO2021257914A1. 2021-12-23.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.1849 mL	5.9246 mL	11.8492 mL	29.6230 mL
	5 mM	0.2370 mL	1.1849 mL	2.3698 mL	5.9246 mL
	10 mM	0.1185 mL	0.5925 mL	1.1849 mL	2.9623 mL
	15 mM	0.0790 mL	0.3950 mL	0.7899 mL	1.9749 mL
	20 mM	0.0592 mL	0.2962 mL	0.5925 mL	1.4811 mL
	25 mM	0.0474 mL	0.2370 mL	0.4740 mL	1.1849 mL
	30 mM	0.0395 mL	0.1975 mL	0.3950 mL	0.9874 mL
	40 mM	0.0296 mL	0.1481 mL	0.2962 mL	0.7406 mL
	50 mM	0.0237 mL	0.1185 mL	0.2370 mL	0.5925 mL
	60 mM	0.0197 mL	0.0987 mL	0.1975 mL	0.4937 mL
	80 mM	0.0148 mL	0.0741 mL	0.1481 mL	0.3703 mL
	100 mM	0.0118 mL	0.0592 mL	0.1185 mL	0.2962 mL