1. PROTAC Immunology/Inflammation
  2. PROTACs IRAK
  3. 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.

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PROTAC IRAK4 degrader-2 Chemical Structure

PROTAC IRAK4 degrader-2 Chemical Structure

CAS No. : 2374122-27-5

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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].

IC50 & Target

IRAK4

 

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.
Molecular Weight

1086.28

Formula

C57H68FN11O8S

CAS No.
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

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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
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PROTAC IRAK4 degrader-2 Related Classifications

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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.

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Product Name:
PROTAC IRAK4 degrader-2
Cat. No.:
HY-135382
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