ML349 is a potent and specific acyl protein thioesterase 2(APT2)/lysophospholipase 2 (LYPLA2) inhibitor with a K_i of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC₅₀ of 144 nM^[1][2].

Ki: 120 nM (APT-2)^[1]
IC50: 144 nM (LYPLA2)^[2]

ML349 is an inhibitor of acyl protein thioesterase 1 and 2 (APT-1 and APT-2) with K_is of >10000 and 120±20 nM, respectively^[1]. ML349 is also an inhibitor of both LYPLA1 and LYPLA2 with IC₅₀s of >3000 and 144 nM, respectivley^[2]. ML348 and ML349 do not decrease cell viability, but they lead to a slight activation of AKT in NRAS mutant cells^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

454.56

C₂₃H₂₂N₂O₄S₂

890819-86-0

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 20 mg/mL (44.00 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: 2 mg/mL (4.40 mM); Suspended solution; Need ultrasonic

  此方案可获得 2 mg/mL (4.40 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• [1]. Won SJ, et al. Molecular Mechanism for Isoform-Selective Inhibition of Acyl Protein Thioesterases 1 and 2 (APT1 and APT2). ACS Chem Biol. 2016 Dec 16;11(12):3374-3382.

  [2]. Adibekian A, et al. Characterization of a Selective, Reversible Inhibitor of Lysophospholipase 2 (LYPLA2).

  [3]. Vujic I, 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.

Cells are plated in 96-well plates with a density of 4000 to 8000 cells per well and incubated for 24 h at 37°C with 5% CO₂. Then cells are treated with increasing drug (including ML349) concentrations and their combinations. Cell viability is measured with the cell viability assay according to the manufacturer’s protocol^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Won SJ, et al. Molecular Mechanism for Isoform-Selective Inhibition of Acyl Protein Thioesterases 1 and 2 (APT1 and APT2). ACS Chem Biol. 2016 Dec 16;11(12):3374-3382.

  [2]. Adibekian A, et al. Characterization of a Selective, Reversible Inhibitor of Lysophospholipase 2 (LYPLA2).

  [3]. Vujic I, 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.