2. PROTAC Immunology/Inflammation Apoptosis
  3. PROTACs IRAK Interleukin Related TNF Receptor
  4. 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

LZ-07 Chemical Structure

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LZ-07 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.

LZ-07 Related Antibodies

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
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2301 mL 6.1507 mL 12.3013 mL
5 mM 0.2460 mL 1.2301 mL 2.4603 mL
View the 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.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

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
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LZ-07 Related Classifications

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:

LZ-07LZ07LZ 07PROTACsIRAKInterleukin RelatedTNF ReceptorInterleukin-1 receptor associated kinaseIL-1R associated kinaseILTumor Necrosis Factor ReceptorTNFRDegraderautoimmunecytokinesInhibitorinhibitorinhibit

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