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ML348
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ML348图片
CAS NO:899713-86-1
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 415.79
Formula C18H17ClF3N3O3
CAS No. 899713-86-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM in DMSO
Water: <1 mg/mL
Ethanol: N/A
SMILES Code O=C(NC1=CC(C(F)(F)F)=CC=C1Cl)CN2CCN(C(C3=CC=CO3)=O)CC2
Synonyms CID 3238952; SID 160654487; ML348; ML-348; ML 348; GNF-Pf-1127; GNF Pf-1127; GNF-Pf 1127
实验参考方法
In Vitro

In vitro activity: ML348 (also known as CID 3238952; SID 160654487) is a reversible inhibitor of LYPLA1 (Lysophospholipase 1) with an IC50 value of 210 nM. It exhibits 14-fold selectivity for LYPLA1 over LYPLA2, ML348 is also selective over a panel of ~30 other serine hydrolases. Protein palmitoylation is an essential post-translational modification necessary for trafficking and localization of regulatory proteins that play key roles in cell growth and signaling. Multiple oncogenes, including HRAS and SRC, require palmitoylation for malignant transformation. LYPLA1 has been identified as a candidate protein palmitoyl thioesterase responsible for HRAS depalmitoylation in mammalian cells.


Kinase Assay: ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor with an IC50 of 210 nM, and barely inhibits LYPLA2


Cell Assay: siRNA mediated knockdown or their inhibition with highly specific inhibitors ML348 and ML349 does not down-regulate NRAS signaling or decrease cell viability. In contrast, palmostatin B showed a dose-dependent reduction of cell viability in a panel of NRAS mutant melanoma cell lines.

In Vivo ML348 (50 mg/kg, i.p., 3 hours) shows potent and selective activity in vivo, inhibits LYPLA1 enzymes in heart, kidney and lung in mice.
Animal model Mice/ C57BL6 male mice
Formulation & Dosage 50 mg/kg, i.p.
References Oncotarget. 2016 Feb 9; 7(6): 7297–7306.