LZ-07
Based on 1 Customer Validation
LZ-07 is a selective IRAK4 PROTAC degrader with DC50 values of 1.14 nM (DOHH2) and 2.70 nM (TMD8). LZ-07 acts as a PI3Kδ kinase inhibitor with an IC50 of 92 nM. By bridging IRAK4 and the CRBN E3 ubiquitin ligase, LZ-07 induces IRAK4 degradation via the ubiquitin-proteasome system, ablates both its kinase and scaffold functions, and thereby blocks downstream inflammatory signal transduction. LZ-07 can be used in research related to autoimmune diseases.
(Pink: IRAK4 ligand (HY-172591); Blue: Cereblon ligand (HY-W883357); Black: linker (HY-B0149)).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.27%
- Fòrmula: C42H48N14O4
- Peso molecular:812.92
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
IRAK4 1.14 nM (DC50, DOHH2) |
IRAK4 2.70 nM (DC50, TMD8) |
PI3Kδ 92 nM (IC50) |
TNF-α |
IL-6 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| TMD8 | DC50 |
2.70 nM
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IRAK4 protein degradation in human TMD8 cells incubated for 16 hrs.
IRAK4 protein degradation in human TMD8 cells incubated for 16 hrs.
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j.cclet.2025.111033 |
| DOHH-2 | DC50 |
1.14 nM
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IRAK4 protein degradation in human DOHH2 cells incubated for 16 hrs.
IRAK4 protein degradation in human DOHH2 cells incubated for 16 hrs.
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j.cclet.2025.111033 |
| PBMC | DC50 |
4.471 nM
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IRAK4 protein degradation in peripheral blood mononuclear cells from healthy donors incubated for 16 hrs.
IRAK4 protein degradation in peripheral blood mononuclear cells from healthy donors incubated for 16 hrs.
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j.cclet.2025.111033 |
| PBMC | IC50 |
6.0 nM
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Inhibition of LPS-induced IL-10 production in peripheral blood mononuclear cells from healthy donor P122071008C pretreated for 2 hrs followed by 24 hrs LPS stimulation, measured via ELISA.
Inhibition of LPS-induced IL-10 production in peripheral blood mononuclear cells from healthy donor P122071008C pretreated for 2 hrs followed by 24 hrs LPS stimulation, measured via ELISA.
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j.cclet.2025.111033 |
| PBMC | IC50 |
6.6 nM
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Inhibition of LPS-induced IL-6 production in peripheral blood mononuclear cells from healthy donor P122071008C pretreated for 2 hrs followed by 24 hrs LPS stimulation, measured via ELISA.
Inhibition of LPS-induced IL-6 production in peripheral blood mononuclear cells from healthy donor P122071008C pretreated for 2 hrs followed by 24 hrs LPS stimulation, measured via ELISA.
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j.cclet.2025.111033 |
| PBMC | IC50 |
4.0 nM
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Inhibition of LPS-induced TNF-α production in peripheral blood mononuclear cells from healthy donor P122071008C pretreated for 2 hrs followed by 24 hrs LPS stimulation, measured via ELISA.
Inhibition of LPS-induced TNF-α production in peripheral blood mononuclear cells from healthy donor P122071008C pretreated for 2 hrs followed by 24 hrs LPS stimulation, measured via ELISA.
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j.cclet.2025.111033 |
| PBMC | IC50 |
2.0 nM
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Inhibition of LPS-induced IL-1β production in peripheral blood mononuclear cells from healthy donor P122071008C pretreated for 2 hrs followed by 24 hrs LPS stimulation, measured via ELISA.
Inhibition of LPS-induced IL-1β production in peripheral blood mononuclear cells from healthy donor P122071008C pretreated for 2 hrs followed by 24 hrs LPS stimulation, measured via ELISA.
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j.cclet.2025.111033 |
| PBMC | IC50 |
>10 μM
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Cytotoxicity against peripheral blood mononuclear cells from healthy donor P122071008C.
Cytotoxicity against peripheral blood mononuclear cells from healthy donor P122071008C.
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j.cclet.2025.111033 |
In Vitro
LZ-07 (0.3-300 nM; 16 h) dose-dependently degrades IRAK4 in TMD8 and DOHH2 cells, with DC50 values of 2.70 nM and 1.14 nM[1].
LZ-07 (30-50 nM; 0.25 h-24 h) rapidly induces IRAK4 degradation in TMD8 and DOHH2 cells, with the maximum degradation achieved at 16 h[1].
LZ-07 (1.52 nM-10 μM; pretreated for 2 h followed by stimulation with LPS (HY-D1056) for 24 h) potently inhibits the secretion of proinflammatory cytokines IL-10, IL-6, TNF-α and IL-1β in PBMCs derived from healthy donors, with IC50 values ranging from 2.0 nM to 6.6 nM[1].
LZ-07 (0.01-1000 nM; 16 h) induces degradation of IRAK4 in PBMCs, with a DC50 of 4.47 nM[1].
LZ-07 (30 nM; 8 h) prevents IRAK4 degradation in TMD8 and DOHH2 cells pretreated with MG132 (HY-13259), MLN4924 (HY-70062), Pomalidomide (HY-10984) or Compound E (HY-14176) due to inhibition of the proteasome or target binding, which demonstrates its dependence on the ubiquitin-proteasome system and dual-target binding[1].
LZ-07 (up to 10 μM) shows no significant cytotoxicity in PBMCs[1].
LZ-07 (0.1-3000 nM) inhibits PI3Kδ kinase activity in cell-free biochemical assays, with an IC50 of 92 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:TMD8 and THP-1 cells
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Concentration:10 nM, 100 nM
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Incubation Time:16 h (TMD8), 24 h (THP-1)
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Result:Significantly degraded more than 65% of the IRAK4 protein at a concentration of 10 nM.
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Cell Line:TMD8 and DOHH2 cells
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Concentration:0.3, 1, 3, 10, 30, 100, 300 nM
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Incubation Time:16 h
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Result:Potently degraded IRAK4 in a dose-dependent manner, with a DC50 of 1.14 nM in DOHH2 cells and 2.70 nM in TMD8 cells.
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Cell Line:TMD8 and DOHH2 cells
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Concentration:50 nM (TMD8), 30 nM (DOHH2)
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Incubation Time:0.25, 0.5, 1, 2, 4, 6, 8, 12, 16, 24 h
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Result:Began to degrade IRAK4 in a short period and reached the maximum degradation rate (Dmax = 91%) at 16 hours.
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Cell Line:TMD8 and DOHH2 cells
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Concentration:30 nmol/L (after 2 hours of pre-treatment with 0.5 μmol/L MG132, 0.5 μmol/L MLN4924, 1 μmol/L Pomalidomide, or 1 μmol/L Compound E)
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Incubation Time:8 h
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Result:The IRAK4 degradation induced by LZ-07 was blocked by the proteasome inhibitor (MG132), ubiquitination inhibitor (MLN4924), and target competitors (Pomalidomide and Compound E), indicating that the degradation relies on the ubiquitin-proteasome system and dual target engagement.
Chemical Information
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Appearance Solid
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Peso molecular 812.92
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Fòrmula C42H48N14O4
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Color Light yellow to green yellow
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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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (123.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2301 mL | 6.1507 mL | 12.3013 mL | 30.7533 mL |
| 5 mM | 0.2460 mL | 1.2301 mL | 2.4603 mL | 6.1507 mL | |
| 10 mM | 0.1230 mL | 0.6151 mL | 1.2301 mL | 3.0753 mL | |
| 15 mM | 0.0820 mL | 0.4100 mL | 0.8201 mL | 2.0502 mL | |
| 20 mM | 0.0615 mL | 0.3075 mL | 0.6151 mL | 1.5377 mL | |
| 25 mM | 0.0492 mL | 0.2460 mL | 0.4921 mL | 1.2301 mL | |
| 30 mM | 0.0410 mL | 0.2050 mL | 0.4100 mL | 1.0251 mL | |
| 40 mM | 0.0308 mL | 0.1538 mL | 0.3075 mL | 0.7688 mL | |
| 50 mM | 0.0246 mL | 0.1230 mL | 0.2460 mL | 0.6151 mL | |
| 60 mM | 0.0205 mL | 0.1025 mL | 0.2050 mL | 0.5126 mL | |
| 80 mM | 0.0154 mL | 0.0769 mL | 0.1538 mL | 0.3844 mL | |
| 100 mM | 0.0123 mL | 0.0615 mL | 0.1230 mL | 0.3075 mL |
LZ-07 Related Classifications
HY-172590 Related Classifications
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