LZ-07
Based on 1 Customer Validation
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).
(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
-
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]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Ver todos los productos específicos de isoformas PROTACs
MoreVer todos los productos específicos de isoformas TNF Receptor
More
Actividad biológica
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.
-
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.
-
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.
Chemical Information
-
Appearance Solid
-
Peso molecular 812.92
-
Fòrmula C42H48N14O4
-
Color Light yellow to green yellow
-
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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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)
Pureza y Documentación
-
Ficha de datos (272 KB)
-
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)
-
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
Powered by Bioz