JH-XII-03-02
Based on 1 Customer Validation
JH-XII-03-02 is a potent and selective LRRK2 PROTAC degrader. JH-XII-03-02 promotes ubiquitination and degradation of LRRK2. JH-XII-03-02 can be used for the research of Parkinson's disease.
(Pink: LRRK2 ligand (HY-177016); Blue: Cereblon ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.33%
- CAS No.: 2415900-86-4
- Formula: C43H51N9O10
- Molecular Weight:853.92
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All PROTACs Isoforms
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Biological Activity
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Cereblon |
JH-XII-03-02 (10-1000 nM; 1-48 h) induces nearly complete degradation of wild-type LRRK2 in MEF cells at 1000 nM after 48 h of treatment, while also potently inhibiting LRRK2 pSer935 phosphorylation[1].
JH-XII-03-02 (1 μM; 48 h) mediates LRRK2 degradation in wild-type MEF cells via a CRBN-dependent ternary complex mechanism, as shown by rescue of degradation with MLi-2 or CRBN degrader pre-treatment[1].
JH-XII-03-02 (1 μM) exhibits excellent kinome selectivity at 1 μM, with no off-target kinases inhibited by more than 85% across a panel of 468 kinases[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Wild-type (WT) mouse embryonic fibroblast (MEF) cells
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Concentration:10-1000 nM
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Incubation Time:1, 6, 24, 48 h
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Result:Induced nearly complete degradation of WT LRRK2 at 1000 nM following 48 h treatment.
Inhibited phosphorylation of LRRK2 pSer935 in a time- and concentration-dependent manner, with significant inhibition observed at 1000 nM after 48 h.
Chemical Information
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CAS No. 2415900-86-4
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Appearance Solid
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Molecular Weight 853.92
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Formula C43H51N9O10
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Color Light yellow to yellow
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SMILES
CC1(CC1)OC2=CC=C(C3=C2)NN=C3C4=NC=NC(N5CCN(C(CCOCCOCCOCCOCCNC6=C7C(C(N(C8C(NC(CC8)=O)=O)C7=O)=O)=CC=C6)=O)CC5)=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (117.11 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)
Purity & Documentation
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Data Sheet (269 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
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 | 1.1711 mL | 5.8553 mL | 11.7107 mL | 29.2767 mL |
| 5 mM | 0.2342 mL | 1.1711 mL | 2.3421 mL | 5.8553 mL | |
| 10 mM | 0.1171 mL | 0.5855 mL | 1.1711 mL | 2.9277 mL | |
| 15 mM | 0.0781 mL | 0.3904 mL | 0.7807 mL | 1.9518 mL | |
| 20 mM | 0.0586 mL | 0.2928 mL | 0.5855 mL | 1.4638 mL | |
| 25 mM | 0.0468 mL | 0.2342 mL | 0.4684 mL | 1.1711 mL | |
| 30 mM | 0.0390 mL | 0.1952 mL | 0.3904 mL | 0.9759 mL | |
| 40 mM | 0.0293 mL | 0.1464 mL | 0.2928 mL | 0.7319 mL | |
| 50 mM | 0.0234 mL | 0.1171 mL | 0.2342 mL | 0.5855 mL | |
| 60 mM | 0.0195 mL | 0.0976 mL | 0.1952 mL | 0.4879 mL | |
| 80 mM | 0.0146 mL | 0.0732 mL | 0.1464 mL | 0.3660 mL | |
| 100 mM | 0.0117 mL | 0.0586 mL | 0.1171 mL | 0.2928 mL |