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Cat. No.: HY-135382

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PROTAC IRAK4 degrader-2

PROTAC IRAK4 degrader-2 (Compound 9) is a PROTAC-based IRAK4 degrader that affords potent IRAK4 degradation with a DC₅₀ in peripheral blood mononuclear cells (PBMCs) cells of 151 nM. PROTAC IRAK4 degrader-2 induce a reduction of IRAK4 protein levels with a DC₅₀ of 36 nM in PBMC cells. PROTAC IRAK4 degrader-2 also leads to the inhibition of multiple cytokines in PBMCs.
(Pink: IRAK4 ligand (HY-19836); Blue: VHL ligand (HY-125845); Black: linker).

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

CAS No.: 2374122-27-5
Formula: C₅₇H₆₈FN₁₁O₈S
Molecular Weight:1086.28

Storage:

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

Data Sheet (269 KB)

PROTAC IRAK4 degrader-2 Chemical Structure

CAS No.: 2374122-27-5

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Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

Description

PROTAC IRAK4 degrader-2 (Compound 9) is a PROTAC-based IRAK4 degrader that affords potent IRAK4 degradation with a DC₅₀ in peripheral blood mononuclear cells (PBMCs) cells of 151 nM. PROTAC IRAK4 degrader-2 induce a reduction of IRAK4 protein levels with a DC₅₀ of 36 nM in PBMC cells. PROTAC IRAK4 degrader-2 also leads to the inhibition of multiple cytokines in PBMCs^[1]. (Pink: IRAK4 ligand (HY-19836); Blue: VHL ligand (HY-125845); Black: linker).

IC₅₀ & Target

IRAK4

All PROTACs Isoforms :

All IRAK Isoforms :

In Vitro

PROTAC IRAK4 degrader-2 (compound 9) (0.01~10 μM; 22 hours; PBMCs) mediated degradation is occurring in a proteasome dependent manner^[1].
PROTAC IRAK4 degrader-2 (compound 9) (0.01~10 μM; 24 hours; PBMCs) induces a reduction of IRAK4 protein levels^[1].

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

Western Blot Analysis^[1]

Cell Line:

PBMCs
Concentration:

0.01, 0.03, 0.1, 0.3, 1, 3 and 10 μM
Incubation Time:

22 and 24 hours
Result:

Induced a reduction of IRAK4 protein levels with a DC₅₀ value of 36 nM and IRAK4 PROTAC-mediated degradation was occurring in a proteasome dependent manner.

Chemical Information

CAS No. 2374122-27-5
Molecular Weight 1086.28
Formula C₅₇H₆₈FN₁₁O₈S
SMILES

COC1=C(C(N)=O)C=C(C(C#CCN2CCC3(CCN(C4=NC=C(C(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)C=N4)CC3)CC2)=CN=C8OC[C@@H]9[C@H](CC)[C@H](F)C(N9)=O)C8=C1
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 (269 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]. Joao Nunes, et al. Targeting IRAK4 for Degradation with PROTACs. ACS Med Chem Lett. 2019 Jun 14;10(7):1081-1085. [Content Brief]

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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.

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100 mg

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

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PROTAC IRAK4 degrader-2

All PROTACs Isoforms

All IRAK Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC IRAK4 degrader-2 Related Classifications

HY-135382 Related Classifications