ABC44
Based on 1 Customer Validation
ABC44 is a potent serine hydrolase inhibitor, with IC50 values of 0.1 μM (HEK293T in situ), 6.5 μM (HEK293T in vitro), and 1.26 μM (cell-free enzymatic assay) against palmitoyl-protein thioesterase 1 (PPT1). ABC44 can be used for research on late infantile neuronal ceroid lipofuscinosis and cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.7%
- CAS. Nr.: 1831135-46-6
- Formel: C31H40N6O5
- Molecular Weight:576.69
-
Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biologische Aktivität
Beschreibung
|
PPT1 0.1 μM (IC50, HEK293T in situ) |
PPT1 6.5 μM (IC50, HEK293T in vitro) |
PPT1 1.26 μM (IC50, cell-free enzymatic assay) |
In Vitro
ABC44 (0.1-5 μM; 1-5 h) significantly inhibits endogenous PPT1 enzyme activity in HepG2 cells and cell lysates[1].
ABC44 (10-20 min) inhibits purified PPT1 with an IC50 of 1.26 μM in a cell-free enzymatic assay[1].
ABC44 (50 µM; 30 min) completely blocks PPT1 substrate hydrolysis activity in hPPT1-transfected HEK293T cell lysates (pH 5.0)[2].
ABC44 (0.001-10 μM; 4 h) exhibits dose-dependent inhibition of endogenous PPT1 activity in HEK293T cells transiently transfected with hPPT1, with an IC50 of 0.1 µM[2].
ABC44 (500 nM; 4 h) inhibits endogenous PPT1 activity in PC3 cells by 90%[2].
ABC44 (0.1-1 μM; 4 h) inhibits endogenous PPT1 activity with high selectivity in isotope-labeled PC3 cells (ABPP-SILAC experiment)[2].
ABC44 exhibits activity inhibiting substrate hydrolysis in hPPT1-transfected HEK293T cell lysates, with an IC50 of 6.5 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HEK293T cells transiently transfected with hPPT1
-
Concentration:200 nM, 2 µM
-
Incubation Time:4 h
-
Result:Inhibited endogenous PPT1 activity in a dose-dependent manner.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57Bl/6[2]
-
Dosage:1 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, and 40 mg/kg
-
Administration:i.p.; single administration; tissues collected 4 hr after dosing
-
Result:Demonstrated potent, dose-dependent in vivo inhibition of PPT1 in both central (brain) and peripheral (e.g., testis) tissues of mice.
At doses of 1 to 5 mg/kg, the product achieved near-complete blockade of PPT1 activity in the tissues.
Chemical Information
-
CAS. Nr. 1831135-46-6
-
Appearance Solid
-
Molecular Weight 576.69
-
Formel C31H40N6O5
-
Color White to off-white
-
SMILES
O=C(N1CCN(C2=CC=C(OC)C=C2)CC1)ON(C3=O)C(N4C3CN(CC5CCN(CC6=CC=CC=C6)CC5)CC4)=O
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 10 mg/mL (17.34 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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
-
Data Sheet (272 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. Puhl AC, et al. Identification of New Modulators and Inhibitors of Palmitoyl-Protein Thioesterase 1 for CLN1 Batten Disease and Cancer. ACS omega. 2024 Mar 12;9(10):11870-11882. [Content Brief]
[2]. Cognetta AB, et al. Selective N-Hydroxyhydantoin Carbamate Inhibitors of Mammalian Serine Hydrolases. Chemistry & biology. 2015 Jul 23;22(7):928-37. [Content Brief]
[3]. Won SJ, et al. Temporal Profiling Establishes a Dynamic S-Palmitoylation Cycle. ACS chemical biology. 2018 Jun 15;13(6):1560-1568. [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 (sealed storage, away from moisture). 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 | 1.7340 mL | 8.6702 mL | 17.3403 mL | 43.3508 mL |
| 5 mM | 0.3468 mL | 1.7340 mL | 3.4681 mL | 8.6702 mL | |
| 10 mM | 0.1734 mL | 0.8670 mL | 1.7340 mL | 4.3351 mL | |
| 15 mM | 0.1156 mL | 0.5780 mL | 1.1560 mL | 2.8901 mL |