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LOM612

Catalog No.GC32921

LOM612 is a potent FOXO relocator, with an EC50 value of 1.5 μM in U2fox RELOC cells.

Products are for research use only. Not for human use. We do not sell to patients.

LOM612 Chemical Structure

Cas No.: 2173232-79-4

Size Price Stock Qty
10mM (in 1mL DMSO)
$354.00
In stock
5mg
$321.00
In stock
10mg
$506.00
In stock
25mg
$1,011.00
In stock
50mg
$1,609.00
In stock
100mg
$2,528.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

Cells are seeded at a concentration of 1× 104 cells/well in 200 μL culture medium and incubated at 37°C in 5% CO2. After 24 hours, when the monolayer formed, the medium is replaced with a final volume of 200 μL of new medium with tested compounds (LOM612, etc.) or controls are added to the plates. Cells are treated with eight 2-fold serial dilutions of each compound spanning concentrations from 50 μM to 0.39 μM in 1% DMSO final. Controls are on the first and the last columns of the plates. On the first column, methyl methanesulfonate (MMS) acts as a positive control and DMSO as a negative control. When compounds (LOM612, etc.) and controls are added, plates are incubated at 37°C in 5% CO2 incubator for 72 hours. After this time, MTT solution is prepared at 5 mg/mL in PBS 1X and then diluted at 0.5 mg/mL in MEM without phenol red. The sample solution in wells is flicked off and 100 μL of MTT dye is added to each well. The plates are gently shaken and incubated for 3 hours at 37°C in 5% CO2 incubator. The supernatant is removed and 100 μL of DMSO 100% is added. The plates are gently shaken to solubilize the formed formazan. The absorbance is measured at a wavelength of 570 nm[1].

References:

[1]. Cautain B, et al. Discovery of a Novel, Isothiazolonaphthoquinone-Based Small Molecule Activator of FOXO Nuclear-Cytoplasmic Shuttling. PLoS One. 2016 Dec 9;11(12):e0167491.

Background

LOM612 is a potent activator of FOXO nuclear translocation, with an EC50 value of 1.5 μM in cells.

LOM612 potently activates nuclear translocation of FOXO with an EC50 value of 1.5 μM, and this effect is independent of CRM-1. LOM612 effectively induces translocation of endogenous FOXO3a and FOXO1, and increases the expression of the FOXO target genes p27 and FasL. LOM612 shows no effect on the nuclear export of endogenous NFKB2 transcription factor in U2OS cells. LOM612 is cytotoxic to HepG2 cells, with an IC50 value of 0.64 μM, and does not sensitize non-cancer THLE2 cells (IC50, 2.76 μM)[1].

[1]. Cautain B, et al. Discovery of a Novel, Isothiazolonaphthoquinone-Based Small Molecule Activator of FOXO Nuclear-Cytoplasmic Shuttling. PLoS One. 2016 Dec 9;11(12):e0167491.

Chemical Properties

Cas No. 2173232-79-4 SDF
Canonical SMILES O=C1C2=C(SN=C2N(C)C)C(C3=CC=CC=C31)=O
Formula C13H10N2O2S M.Wt 258.3
Solubility DMSO : 6 mg/mL (23.23 mM);Water : < 0.1 mg/mL (insoluble) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.8715 mL 19.3573 mL 38.7147 mL
5 mM 0.7743 mL 3.8715 mL 7.7429 mL
10 mM 0.3871 mL 1.9357 mL 3.8715 mL
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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 3 reference(s) in Google Scholar.)

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