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ML348
Axon 2646
CAS:
899713-86-1
Purity:
99%
- Soluble in DMSO
- MF: C18H17ClF3N3O3
- MW: 415.79
Description
ML348 is a selective and in vivo active inhibitor for acyl-protein thioesterase APT1（LYPLA1) with Ki of 280 nM. It displays significant isoform selectivity over APT2 (LYPLA2) with Ki >10 µM. ML348 is a useful tool to study LYPLA/APT mediated protein S-palmitoylation and related pharmacology.
APT1 pharmacology plays a critical role in translational and disease-focused cellular models. ML348 serves as a valuable tool for mechanistic studies, facilitating the evaluation of APT1 (LYPLA1) activity across biochemical, cellular, and pathological assays.
Key Features
- APT1 inhibitor
- High APT1 Isoform Selectivity over APT2
- A competitive inhibitor that binds directly within the putative acyl-binding pocket of APT1
- Prevents the depalmitoylation of S-acylated proteins
Applications
- APT1 pharmacology and target-validation studies
- Neurodegenerative Disease Research
- Oncogenic Signaling Studies
- Metabolic pathway and biomarker-response studies
More Information
| Parent CAS No. | 899713-86-1 |
|---|---|
| Chemical Name | N-(2-chloro-5-(trifluoromethyl)phenyl)-2-(4-(furan-2-carbonyl)piperazin-1-yl)acetamide |
| SMILES | N1(CC(NC2=CC(C(F)(F)F)=CC=C2Cl)=O)CCN(C(C2=CC=CO2)=O)CC1 |
| MFCD | N.A. |
| InChi | InChI=1S/C18H17ClF3N3O3/c19-13-4-3-12(18(20,21)22)10-14(13)23-16(26)11-24-5-7-25(8-6-24)17(27)15-2-1-9-28-15/h1-4,9-10H,5-8,11H2,(H,23,26) |
| InChiKey | OXKNHBBDOIMFFQ-UHFFFAOYSA-N |
| CID | 3238952 |
| Short Description | APT1 inhibitor |
ML348
selective APT1/LYPLA1 inhibitor
ML-348
S-palmitoylated proteins
LYPLA
APT2
LYPLA1
LYPLA2
APT1/LYPLA1
acyl-protein thioesterase
Inhibitor
APT1 pharmacology
Neurodegenerative Disease Research
Oncogenic Signaling Studies
Metabolic pathway and biomarker-response studies
neurodegeneration
metabolism
receptor selectivity
signal transduction
enzyme pharmacology
drug discovery
CAS 899713-86-1
Axon Medchem
Axon 2646
Supplier
Vendor
References
- I Vujic et al. Acyl protein thioesterase 1 and 2 (APT-1, APT-2) inhibitors palmostatin B, ML348 and ML349 have different effects on NRAS mutant melanoma cells. Oncotarget. 2016 Feb 9;7(6):7297-306.
- JJ Hulce et al. An in Vivo Active Carbamate-based Dual Inhibitor of Lysophospholipase 1 (LYPLA1) and Lysophospholipase 2 (LYPLA2). Probe Reports from the NIH Molecular Libraries Program. Bethesda (MD): NCBI (US); 2010-2013 Dec 09
- SJ Won et al. Molecular Mechanism for Isoform-Selective Inhibition of Acyl Protein Thioesterases 1 and 2 (APT1 and APT2). ACS Chem Biol. 2016 Oct 31.
- A Adibekian et al. Confirming target engagement for reversible inhibitors in vivo by kinetically tuned activity-based probes. J Am Chem Soc. 2012 Jun 27;134(25):10345-8.
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