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CAS No.: 899713-86-1

ML348 Catalog No. CSN18844

Synonyms: GNF-Pf-1127;CID 3238952;SID 160654487

ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor (IC50 = 210 nM), Exhibits 14-fold selectivity for LYPLA1 over LYPLA2, Also selective over a panel of ~30 other serine hydrolases.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Protein palmitoylation, an important post-translational modification necessary for trafficking and localization of regulatory proteins, plays key roles in cell growth and signaling. Palmitoylation is required for malignant transformation of multiple oncogenes, including HRAS and SRC. Lysophospholipase 1 (LYPLA1) has been confirmed as a palmitoyl thioesterase that is responsible for HRAS depalmitoylation in mammalian cells. ML348 is a selective and reversible LYPLA1 inhibitor with IC50 value of 210 nM and K_i value of 280 nM. ML348 showed no cytotoxic effects on human embryonic kidney cells (HEK293T). Maximum soluble drug concentrations of ML348 treatment (<12.5 μM) did not decrease cell viability, but led to a slight activation of AKT in NRAS mutant cells.
作用机制ML348 inhibits LYPLA1 by occupying a putative acyl-binding region, establishing the mechanism for isoform-specific inhibition and hydrolysis of acyl substrates.
动物研究
剂量
Mice: 50 mg/kg^[1] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 50 mg/kg^[1] (i.p.)
给药途径	i.p.

[1] Characterization of a Selective, Reversible Inhibitor of Lysophospholipase 2 (LYPLA2)

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4050 mL
- 12.0252 mL
- 24.0504 mL
- 5 mM
- 0.4810 mL
- 2.4050 mL
- 4.8101 mL
- 10 mM
- 0.2405 mL
- 1.2025 mL
- 2.4050 mL

技术信息

CAS号

899713-86-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H17ClF3N3O3

运输

蓝冰

分子量

415.79

别名

GNF-Pf-1127;CID 3238952;SID 160654487

溶解度

DMSO	40.0 mg/mL (96.2 mM)
Water	insoluble

动物实验配方

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