2. PROTAC Immunology/Inflammation
  3. PROTACs IRAK
  4. PROTAC IRAK3 degrader-1

PROTAC IRAK3 degrader-1 is a potent and selective IRAK3 degrader with a DC50 of 0.002 μM. PROTAC IRAK3 degrader-1 induces proteasome-dependent degradation of IRAK3 via ternary complex formation with IRAK3 and CRBN. PROTAC IRAK3 degrader-1 can be used for cancer research.
(Pink: IRAK3 Target protein ligand; Blue: Cereblon ligand (HY-14658); Black: linker).

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

PROTAC IRAK3 degrader-1

PROTAC IRAK3 degrader-1 Chemical Structure

CAS No. : 2712600-00-3

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.

Other In-stock Forms of PROTAC IRAK3 degrader-1:

Other Forms of PROTAC IRAK3 degrader-1:

PROTAC IRAK3 degrader-1 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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC IRAK3 degrader-1 is a potent and selective IRAK3 degrader with a DC50 of 0.002 μM. PROTAC IRAK3 degrader-1 induces proteasome-dependent degradation of IRAK3 via ternary complex formation with IRAK3 and CRBN. PROTAC IRAK3 degrader-1 can be used for cancer research[1]. (Pink: IRAK3 Target protein ligand; Blue: Cereblon ligand (HY-14658); Black: linker).

IC50 & Target[1]

IRAK3

5 nM (IC50)

IRAK4

1.4 μM (IC50)

In Vitro

PROTAC IRAK3 degrader-1 (compound 23) potently and selectively binds to recombinant IRAK3 with an IC50 of 5 nM, with 280-fold selectivity over IRAK4[1].
PROTAC IRAK3 degrader-1 binds to recombinant CRBN with an IC50 of 460 nM[1].
PROTAC IRAK3 degrader-1 shows primary selectivity for recombinant IRAK3 in a 400-kinase panel, with weaker inhibition of CDK11, CDK8, TRKC, and GSG2[1].
PROTAC IRAK3 degrader-1 selectively binds to IRAK3 in a chemoproteomic assay, with an apparent binding constant of 34 nM and >20-fold selectivity over all other detected targets[1].
PROTAC IRAK3 degrader-1 (0.0003-10 μM; 2-48 h) potently degrades IRAK3 in THP1 cells, sustained degradation[1].
PROTAC IRAK3 degrader-1 (0.1 μM; 8 h) selectively decreases IRAK3 protein levels in THP1 cells, with only minimal off-target effects on DHCR24 and no degradation of IKZF1, GSPT1, IRAK1, or IRAK4[1].
PROTAC IRAK3 degrader-1 (0.3 μM; 8-32 h) induces significant, sustained IRAK3 degradation in primary human macrophages, and this activity is unaffected by LPS stimulation[1].

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

PROTAC IRAK3 degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: THP1 monocytic cancer cells
Concentration: 0.0003; 0.001; 0.003; 0.01; 0.03; 0.1; 0.3; 1; 3; 10 μM
Incubation Time: 2; 4; 6; 8; 16; 24; 48 h
Result: Induced potent IRAK3 degradation with a DC50 of 2 nM and maximum degradation (Dmax) of 98% after 16 h.
Achieved maximal degradation at 0.1 μM after 24 h.
Detected degradation as early as 2 h after treatment with 0.1 μM, which persisted up to 48 h.
Allowed full IRAK3 recovery 24 h after compound washout.

Western Blot Analysis[1]

Cell Line: THP1 monocytic cancer cells
Concentration: 0.1; 0.3; 1; 3; 10 μM
Incubation Time: 6; 24 h
Result: Fully rescued IRAK3 degradation when cells were pretreated with proteasome inhibitor MG132 or NEDD8-activating enzyme inhibitor MLN4924.
Prevented IRAK3 degradation when cells were pretreated with excess IRAK3 ligand 5 or thalidomide.
Molecular Weight

878.07

Formula

C47H63N11O6
CAS No.
SMILES

O=C1C2=CC(N3CCN(CC3)CCC4CCN(CC4)C(CCC(N5CCN([C@@]6([H])CC[C@H](CC6)NC7=NC=NN8C7=C(C(C)C)C=C8)CC5)=O)=O)=CC=C2C(N1C9C(NC(CC9)=O)=O)=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 IRAK3 degrader-1 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 IRAK3 degrader-12712600-00-3PROTACsIRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseubiquitin-proteasome pathwayTHP1 cellsIRAK3CRBNIRAK4primary human macrophagesCDK8proteasome-dependent degradationternary complexCDK11Inhibitorinhibitorinhibit

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 IRAK3 degrader-1
Cat. No.:
HY-142662
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.