2. PROTAC Immunology/Inflammation NF-κB MAPK/ERK Pathway
  3. PROTACs IRAK NF-κB p38 MAPK
  4. GSI526

GSI526 is a IRAK4 PROTAC degrader (DC50=40.17 nM, Dmax=97%; THP-1) based on the VHL ubiquitin-proteasome system. GSI526 inhibits IRAK4-mediated NF-κB and MAPK inflammatory signaling pathways, and induces IRAK4 degradation in myeloid cells. GSI526 is applicable to inflammation-related research.
(Pink: IRAK4 ligand (HY-183800); Blue: VHL ligand (HY-112078); Black: linker).

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

GSI526

GSI526 Chemical Structure

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GSI526 Related Antibodies

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Description

GSI526 is a IRAK4 PROTAC degrader (DC50=40.17 nM, Dmax=97%; THP-1) based on the VHL ubiquitin-proteasome system. GSI526 inhibits IRAK4-mediated NF-κB and MAPK inflammatory signaling pathways, and induces IRAK4 degradation in myeloid cells. GSI526 is applicable to inflammation-related research[1]. (Pink: IRAK4 ligand (HY-183800); Blue: VHL ligand (HY-112078); Black: linker).

IC50 & Target[1]

VHL

 

IRAK4

 

In Vitro

GSI526 (1-10000 nM; 24 h) induces dose-dependent degradation of IRAK4 in HEK293T cells with a DC50 of 50.89 nM and a Dmax greater than 80%[1].
GSI526 (0.01-30 μM; 24 h) exhibits no cytotoxicity in THP-1 cells at concentrations up to 30 μM following 24 h incubation[1].
GSI526 (0.01-30 μM; 48 h) exhibits no cytotoxicity in HEK293T cells at concentrations up to 30 μM following 48 h incubation[1].
GSI526 (1000 nM; 8 h) exhibits marked selectivity toward IRAK4 in THP-1 cells, with IRAK4 showing a statistically significant downregulation following 8 h treatment with 1000 nM GSI526[1].
GSI526 (1-5 μM; 1 h pretreatment, followed by 6 h LPS stimulation) inhibits LPS-induced activation of the IRAK4-NF-κB/MAPK signaling pathway in THP-1 cells via degradation of IRAK4[1].
GSI526 (0.3-3 μM; 1 h pretreatment, followed by 24 h LPS stimulation) dose-dependently inhibits LPS-induced expression of TNF-α and CXCL8 in THP-1 cells via suppression of the IRAK4-NF-κB/MAPK signaling pathway[1].

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

GSI526 Related Antibodies

Western Blot Analysis[1]

Cell Line: THP-1 human monocytic leukemia cells
Concentration: 1-10000 nM (dose-response); 1 μM (time-course)
Incubation Time: 24 h (dose-response); 2-24 h (time-course)
Result: Induced dose-dependent degradation of IRAK4 with a DC50 of 40.17 nM and a maximum degradation (Dmax) of 97%.
Resulted in detectable IRAK4 degradation within 2 h, with maximal degradation achieved by 8 h, and the degradative effect was sustained for up to 24 h.

Western Blot Analysis[1]

Cell Line: HEK293T human embryonic kidney cells
Concentration: 1-10000 nM
Incubation Time: 24 h
Result: Induced dose-dependent degradation of IRAK4 with a DC50 of 50.89 nM and a Dmax greater than 80%.

Cell Viability Assay[1]

Cell Line: THP-1 human monocytic leukemia cells
Concentration: 0.01-30 μM
Incubation Time: 24 h
Result: Did not induce cytotoxic cell death at concentrations up to 30 μM.

Cell Viability Assay[1]

Cell Line: HEK293T human embryonic kidney cells
Concentration: 0.01-30 μM
Incubation Time: 48 h
Result: Did not induce cytotoxic cell death at concentrations up to 30 μM.

Western Blot Analysis[1]

Cell Line: THP-1 human monocytic leukemia cells
Concentration: 1-5 μM
Incubation Time: 1 h pretreatment, followed by 6 h LPS stimulation
Result: Inhibited LPS-induced phosphorylation of JNK, p38, ERK, and p65 (NF-κB) in a concentration-dependent manner via IRAK4 degradation.

Real Time qPCR[1]

Cell Line: THP-1 human monocytic leukemia cells
Concentration: 0.3-3 μM
Incubation Time: 1 h pretreatment, followed by 24 h LPS stimulation
Result: Significantly inhibited LPS-induced secretion of pro-inflammatory cytokine TNF-α and chemokine CXCL8, with the inhibitory effect particularly evident at 1 and 3 μM.
Molecular Weight

959.17

Formula

C51H62N10O7S
SMILES

O=C(C1=NC(C2=CC=NN2)=CC=C1)NC3=C(OC)C=C(N4CCC5(CN(C(CCCC(N[C@@H](C(C)(C)C)C(N6[C@H](C(N[C@@H](C)C7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C6)=O)=O)=O)C5)CC4)C=C3
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
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GSI526 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.

Keywords:

GSI526GSI 526GSI-526PROTACsIRAKNF-κBp38 MAPKInterleukin-1 receptor associated kinaseIL-1R associated kinaseNuclear factor-κBNuclear factor-kappaBMAPKmyeloid cellsTHP-1 cellsIRAK4VHLubiquitin-proteasome systemHEK293T cellsinterleukin-1 receptor-associated kinase 4TNF-αInhibitorinhibitorinhibit

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