1. PROTAC Immunology/Inflammation Apoptosis
  2. PROTACs IRAK Interleukin Related TNF Receptor
  3. LZ-07

LZ-07 is a IRAK4 PROTAC degrader (DC50 = 1.14 nM). LZ-07 leads to marked suppression of cytokines including IL-6, IL-1β, TNF-α, and IL-10 upon degradation of IRAK4. LZ-07 can be studied in research for autoimmune diseases (Pink: IRAK4 ligand (HY-172591); Blue: CRBN ligand (HY-34590); Black: linker (HY-B0149); CRBN ligand + linker: HY-172593).

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

LZ-07 Chemical Structure

LZ-07 Chemical Structure

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Description

LZ-07 is a IRAK4 PROTAC degrader (DC50 = 1.14 nM). LZ-07 leads to marked suppression of cytokines including IL-6, IL-1β, TNF-α, and IL-10 upon degradation of IRAK4. LZ-07 can be studied in research for autoimmune diseases (Pink: IRAK4 ligand (HY-172591); Blue: CRBN ligand (HY-34590); Black: linker (HY-B0149); CRBN ligand + linker: HY-172593)[1].

In Vitro

LZ-07 (10-100 nM, 16 h) displays the strongest degradation activity with degradation levels exceeding 65% at 10 nM and >75% at 100 nM in THP-1 cells[1].
LZ-07 (0.3-300 nM, 16 h) demonstrates dose-dependent IRAK4 degradation in DOHH2 and TMD8 cells (DC50 of 1.14 nM and 2.70 nM)[1].
LZ-07 (0.3-300 nM, 0-24 h) induces rapid and significant degradation within 4 h at 50 nM, achieving maximum degradation at 16 h in TMD8 cells (Dmax = 91%) and degrades IRAK4 in DOHH2 cells rapidly[1].
LZ-07 (30 nM, 8 h) mediates IRAK4 degradation through the ubiquitin-proteasome system and that its activity depends on the binding to both IRAK4 and CRBN[1].
LZ-07 (3.9-7.6 nM, 2 h) demonstrates superior inhibition of four key inflammatory cytokines (IL-6, IL-10, IL-1β and TNF-α) in LPS (100 ng/mL)-stimulated PBMCs[1].

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

Western Blot Analysis[1]

Cell Line: Pretreated DOHH2 and TMD8 cells with DMSO, MG132 (HY-13259) (0.5 μM), MLN4924 (HY-70062) (0.5 μM), Pomalidomide (HY-10984) (1 μM) and Compound E (1 μM)
Concentration: 30 nM
Incubation Time: 8 h
Result: Inhibited IRAK4 degradation and the degradation was blocked by pretreatment of proteasome inhibitor MG132, the ubiquitination inhibitor MLN4924, compound E and pomalidomide.

ELISA Assay[1]

Cell Line: LZ-07 pretreated PBMCs with LPS stimulation (100 ng/mL)
Concentration: 3.9-7.6 nM
Incubation Time: 2 h pretreatment, followed by stimulation with LPS for 24 h
Result: Exhibited 131-fold greater inhibition of IL-6 compared to KT-474 (HY-145483) in PBMCs from one healthy donor.
Inhibited IL-6 with an IC50 of 4.8 nM in PBMC from another donor.
Inhibited key inflammatory cytokines including IL-6, IL-10, IL-1β and TNF-α.
Molecular Weight

812.92

Formula

C42H48N14O4

SMILES

CC1(CC1)NC2=NC(NC3=CN(C4CCN(C([C@@H]5CC[C@@H](CNC6=CN=C(C(NC7CCC(NC7=O)=O)=O)C=C6)CC5)=O)CC4)N=C3)=NC8=CC=C(C9=CN=CN=C9)N=C82

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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
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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:
LZ-07
Cat. No.:
HY-172590
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