JYQ-164
Based on 1 Customer Validation
JYQ-164 is a cell-permeable covalent PARK7 inhibitor (human IC50 = 21 nM). JYQ-164 covalently modifies the key active-site cysteine and inhibits PARK7 enzymatic activity, shows selectivity for PARK7 in cysteine-activity-based proteomic profiling, and does not interfere with deubiquitinase activities including UCHL1. JYQ-164 can be used for PARK7-related research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.43%
- CAS. Nr.: 3117543-49-1
- Formel: C23H26N6O5S2
- Molecular Weight:530.62
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PARK7 21 nM (IC50) |
In Vitro
JYQ-164 (0.001-100 μM; 1 h) inhibits PARK7 glyoxalase activity in the DiFMUAc assay with an IC50 of 21 nM[1].
JYQ-164 (15 μM; 1 h) covalently modifies PARK7 as detected by intact-protein LC-MS[1].
JYQ-164 (0.1-5 μM; 24 h) binds to endogenous PARK7 in live HEK293T cells in a competition assay, starting from 0.1 μM after 24 h[1].
JYQ-164 (0.5-5 μM; 4 h) selectively targets PARK7 Cys106 in A549 cells, with DBIA labeling reduced by ≥ 75% after 4 h at 5 μM, whereas no ≥ 75% target reduction is observed at 0.5 μM[1].
JYQ-164 (0.25-1.25 µM; 1-2 h) is an HTS-derived, FP-validated PARK7 screening hit from a 471-member cyanoamide compound library[2].
JYQ-164 (0.25-1 µM) effectively binds recombinant PARK7 in the FP assay at 0.25 µM with > 95% inhibition[2].
JYQ-164 (0.001-100 µM; 1 h) inhibits recombinant PARK7 enzyme activity with an IC50 of 21 nM and 861-fold selectivity over UCHL1[2].
JYQ-164 (15 µM; 1 h) forms a covalent complex with recombinant PARK7 as detected by intact-protein LC-MS[2].
JYQ-164 (0.1-5 µM; 24 h) is cell-permeable and binds to PARK7 in HEK293T cells starting at 0.1 µM[2].
JYQ-164 (24 h) does not interfere with DUB activity in HEK293T cells[2].
JYQ-164 (0.5-5 µM; 4 h) selectively targets PARK7 Cys106 at 5 µM in A549 cells in SLC-ABPP proteomics[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:0.5 μM; 1 μM; 2.5 μM; 5 μM
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Incubation Time:72 h (renewed at 36 h)
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Result:Did not show cytotoxicity in A549 cells up to 5 μM after 72 h, but still showed complete inhibition of PARK7 engagement with the JYQ-92 probe.
Chemical Information
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CAS. Nr. 3117543-49-1
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Appearance Solid
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Molecular Weight 530.62
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Formel C23H26N6O5S2
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Color White to off-white
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SMILES
O=C([C@H]1CN(C#N)CC1)NC(S2)=NC3=C2CN(C(C4=CC=CC(S(=O)(N5CCOCC5)=O)=C4)=O)CC3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 50 mg/mL (94.23 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Jia Y, et al. Development of Inhibitors, Probes, and PROTAC Provides a Complete Toolbox to Study PARK7 in the Living Cell. Journal of medicinal chemistry. 2024 May 23;67(10):7935-7953. [Content Brief]
[2]. Jia Y, et al. Development of potent and cell-permeable chemical tools for PARK7. [Content Brief]
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 | 1.8846 mL | 9.4229 mL | 18.8459 mL | 47.1147 mL |
| 5 mM | 0.3769 mL | 1.8846 mL | 3.7692 mL | 9.4229 mL | |
| 10 mM | 0.1885 mL | 0.9423 mL | 1.8846 mL | 4.7115 mL | |
| 15 mM | 0.1256 mL | 0.6282 mL | 1.2564 mL | 3.1410 mL | |
| 20 mM | 0.0942 mL | 0.4711 mL | 0.9423 mL | 2.3557 mL | |
| 25 mM | 0.0754 mL | 0.3769 mL | 0.7538 mL | 1.8846 mL | |
| 30 mM | 0.0628 mL | 0.3141 mL | 0.6282 mL | 1.5705 mL | |
| 40 mM | 0.0471 mL | 0.2356 mL | 0.4711 mL | 1.1779 mL | |
| 50 mM | 0.0377 mL | 0.1885 mL | 0.3769 mL | 0.9423 mL | |
| 60 mM | 0.0314 mL | 0.1570 mL | 0.3141 mL | 0.7852 mL | |
| 80 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.5889 mL |
JYQ-164 Related Classifications
HY-163562 Related Classifications
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