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Cat. No.: HY-181708

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PROTAC IRAK4 degrader-14

PROTAC IRAK4 degrader-14 is an orally active IRAK4 PROTAC degrader with a DC₅₀ of 2.4 nM. PROTAC IRAK4 degrader-14 inhibits proinflammatory responses in multiple cell types including T cells, monocytes and keratinocytes. PROTAC IRAK4 degrader-14 is applicable to research related to psoriasis.
(Pink: IRAK4 ligand (HY-19836); Blue: MDM2 ligand (HY-N0004); Black: linker).

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

CAS No.: 3113890-51-7
Formula: C₅₉H₆₈FN₅O₁₃
Molecular Weight:1074.20

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

PROTAC IRAK4 degrader-14 Chemical Structure

CAS No.: 3113890-51-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC IRAK4 degrader-14 is an orally active IRAK4 PROTAC degrader with a DC₅₀ of 2.4 nM. PROTAC IRAK4 degrader-14 inhibits proinflammatory responses in multiple cell types including T cells, monocytes and keratinocytes. PROTAC IRAK4 degrader-14 is applicable to research related to psoriasis^[1]. (Pink: IRAK4 ligand (HY-19836); Blue: MDM2 ligand (HY-N0004); Black: linker).

IC₅₀ & Target^[1]

IRAK4

2.4 nM (DC₅₀)

IL-6

IL-2

All PROTACs Isoforms :

All IRAK Isoforms :

All TNF Receptor Isoforms :

All Interleukin Related Isoforms :

All CXCR Isoforms :

All CCR Isoforms :

In Vitro

PROTAC IRAK4 degrader-14 (Compound Ori-Zim-6) (250 nM; 3-24 h) induces time-dependent IRAK4 degradation in human monocytic THP-1 cells, achieving >90% degradation within 12 h and complete degradation by 24 h when treated at 250 nM^[1].
PROTAC IRAK4 degrader-14 (250-500 nM; 12-24 h) induces proteasome-dependent, NCL- and MDM2-dependent ubiquitination and degradation of IRAK4, and promotes assembly of an MDM2-NCL-PROTAC-IRAK4 quaternary complex in human monocytic THP-1 cells^[1].
PROTAC IRAK4 degrader-14 (0.01-1 μM; 24 h) concentration-dependently inhibits LPS-induced pro-inflammatory mediator (CCL2, CXCL8, IL-6, TNF-α) mRNA expression in human monocytic THP-1 cells^[1].
PROTAC IRAK4 degrader-14 (0.01-1 μM; 24 h) concentration-dependently inhibits pro-inflammatory cytokine (TNF-α, IL-2, IFN-γ) mRNA expression in human Jurkat T cells^[1].
PROTAC IRAK4 degrader-14 (0.01-1 μM; 24 h) concentration-dependently inhibits IL-1β-induced pro-inflammatory mediator (TNF-α, IL-6, CXCL8, IL-19) mRNA expression in human keratinocyte HaCaT cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR^[1]

Cell Line:

LPS-Stimulated Human Monocytic THP-1 Cells
Concentration:

0.01, 0.1 and 1 μM
Incubation Time:

24 h
Result:

Caused concentration-dependent reductions in mRNA levels of pro-inflammatory mediators CCL2, CXCL8, IL-6, and TNF-α.
Exhibited more potent inhibition of CCL2, IL-6, and TNF-α mRNA expression than the reference degrader KT-474 at equivalent concentrations.

Real Time qPCR^[1]

Cell Line:

Human Jurkat T Cells
Concentration:

0.01, 0.1 and 1 μM
Incubation Time:

24 h
Result:

Suppressed T cell activation via reduced mRNA levels of TNF-α, IL-2, and IFN-γ.
Exhibited more potent suppression of IFN-γ mRNA than KT-474 at equivalent concentrations.

Real Time qPCR^[1]

Cell Line:

IL-1β-Stimulated Human Keratinocyte HaCaT Cells
Concentration:

0.01-1 μM
Incubation Time:

24 h
Result:

Suppressed mRNA levels of TNF-α, IL-6, CXCL8, and IL-19.
Exhibited stronger suppression of IL-6, CXCL8, and IL-19 mRNA levels than KT-474 at equivalent concentrations.

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_0-t	AUC_0-∞	T_1/2	CL	V_ss	F
Mice^[1]	2 mg/kg	i.v.	0.13 h	174.32 ng/mL	452.38 ng·h/mL	549.32 ng·h/mL	5.1 h	60.67 mL/min/kg	24 L/kg	/
Mice^[1]	20 mg/kg	p.o.	0.25 h	73.18 ng/mL	233.51 ng·h/mL	264.66 ng·h/mL	4.0 h	75.36 mL/min/kg	420 L/kg	5 %

In Vivo

PROTAC IRAK4 degrader-14 (Compound Ori-Zim-6) (20 mg/kg; p.o.; once daily for 5 consecutive days) exhibits significant efficacy in an Imiquimod (IMQ) (HY-B0180)-induced psoriasis mouse model, along with favorable safety profiles including recovery of body weight and serum liver function parameters^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c
(male, 6-8 weeks old)^[1]
Dosage:

20 mg/kg
Administration:

p.o.; daily; 5 consecutive days
Result:

Reduced total Psoriasis Area and Severity Index (PASI) scores, ear thickening, spleen enlargement, and dorsal skin epidermal thickness.
Downregulated mRNA expression of IL-1β, IL-23, Lipocalin-2 (Lcn2), and TNF-α in ear skin tissues.
Prevented IMQ-induced body weight loss.
Significantly restored serum albumin (ALB) and alkaline phosphatase (ALP) levels.
Showed no detectable histopathological damage to major organs (heart, liver, spleen, lung, kidney).

Chemical Information

CAS No. 3113890-51-7
Molecular Weight 1074.20
Formula C₅₉H₆₈FN₅O₁₃
SMILES

O=C(O[C@H]([C@H]1CC[C@]23[H])[C@]2(C(C1=C)=O)[C@]4(O)OC[C@@]53[C@@H](O)CCC([C@@]5([H])[C@@H]4O)(C)C)CCC(N6CCC7(CCN(CC7)C(C8=CC=C(C#CC9=CN=C(OC[C@H]([C@@H]%10CC)NC([C@H]%10F)=O)C%11=CC(OC)=C(C(N)=O)C=C9%11)C=C8)=O)C6)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Feng Z, et al. Design, Synthesis, and Evaluation of Nucleolin-Bridged, MDM2-Recruiting IRAK4 Degraders for the Treatment of Autoimmune Diseases. J Med Chem. 2026;69(4):4855-4872. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

MOQ

Minimum order quantity

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PROTAC IRAK4 degrader-14

All PROTACs Isoforms

All IRAK Isoforms

All TNF Receptor Isoforms

All Interleukin Related Isoforms

All CXCR Isoforms

All CCR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC IRAK4 degrader-14 Related Classifications

HY-181708 Related Classifications