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> ML349 [890819-86-0]

ML349 [890819-86-0]

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

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ML349 Estructura química

ML349 Estructura química

No. CAS : 890819-86-0

This product is a controlled substance and not for sale in your territory.

Based on 1 publication(s) in Google Scholar

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Descripciòn

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

IC50 & Target

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

ML349 is an inhibitor of acyl protein thioesterase 1 and 2 (APT-1 and APT-2) with Kis? 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ML349 Related Antibodies
Peso molecular

454.56

Fòrmula

C23H22N2O4S2
No. CAS

890819-86-0
Appearance

Solid

Color

White to yellow

SMILES

COC1=CC=C(N2CCN(C(C3=CC4=C(C(C=CC=C5)=C5S(C4)(=O)=O)S3)=O)CC2)C=C1
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

DMSO : 20 mg/mL (44.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1999 mL 10.9996 mL 21.9993 mL
5 mM 0.4400 mL 2.1999 mL 4.3999 mL
View the 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación

Purity: 99.40%

COA (249 KB) HNMR (269 KB) RP-HPLC (212 KB) MS (73 KB)

Instrucciones de manejo (2659 KB)
Referencias

  • [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.  [Content Brief]

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

    [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.  [Content Brief]

Ensayo celular
[3]

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].

MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias

  • [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.  [Content Brief]

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

    [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.  [Content Brief]

  • [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.

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. 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 2.1999 mL 10.9996 mL 21.9993 mL 54.9982 mL
5 mM 0.4400 mL 2.1999 mL 4.3999 mL 10.9996 mL
10 mM 0.2200 mL 1.1000 mL 2.1999 mL 5.4998 mL
15 mM 0.1467 mL 0.7333 mL 1.4666 mL 3.6665 mL
20 mM 0.1100 mL 0.5500 mL 1.1000 mL 2.7499 mL
25 mM 0.0880 mL 0.4400 mL 0.8800 mL 2.1999 mL
30 mM 0.0733 mL 0.3667 mL 0.7333 mL 1.8333 mL
40 mM 0.0550 mL 0.2750 mL 0.5500 mL 1.3750 mL
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ML349 Related Classifications

Help & FAQs

Keywords:

ML349890819-86-0ML 349ML-349PhospholipaseInhibitorinhibitorinhibit