2. PROTAC Immunology/Inflammation Apoptosis GPCR/G Protein
  3. PROTACs IRAK TNF Receptor IFNAR Interleukin Related CXCR CCR
  4. 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.

PROTAC IRAK4 degrader-14

PROTAC IRAK4 degrader-14 Chemical Structure

CAS No. : 3113890-51-7

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

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

PROTAC IRAK4 degrader-14 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All IRAK Isoform Specific Products:

View All Isoforms
IRAK1 IRAK3 IRAK4

View All TNF Receptor Isoform Specific Products:

View All Isoforms
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

View All Interleukin Related Isoform Specific Products:

View All Isoforms
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

View All CXCR Isoform Specific Products:

View All Isoforms
CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

View All CCR Isoform Specific Products:

View All Isoforms
CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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

 

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.

PROTAC IRAK4 degrader-14 Related Antibodies

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 Tmax Cmax AUC0-t AUC0-∞ T1/2 CL Vss 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).
Molecular Weight

1074.20

Formula

C59H68FN5O13
CAS No.
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
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PROTAC IRAK4 degrader-14 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC IRAK4 degrader-143113890-51-7PROTACsIRAKTNF ReceptorIFNARInterleukin RelatedCXCRCCRInterleukin-1 receptor associated kinaseIL-1R associated kinaseTumor Necrosis Factor ReceptorTNFRInterferon-α/β receptorInterferon-alpha/beta receptor ILCXC chemokine receptorsC-X-C motif chemokine receptorsCC chemokine receptorpsoriasisubiquitin-proteasome systemIRAK4Jurkat T cellsnucleolinTHP-1 cellsT cellsMDM2monocyteskeratinocytesInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PROTAC IRAK4 degrader-14
Cat. No.:
HY-181708
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.