2. Metabolic Enzyme/Protease
  3. Glutathione S-transferase
  4. GSTO1-IN-1

GSTO1-IN-1 is a potent glutathione S-transferase omega 1 (GSTO1) inhibitor with an IC50 of 31 nM.

For research use only. We do not sell to patients.

GSTO1-IN-1 Chemical Structure

GSTO1-IN-1 Chemical Structure

CAS No. : 568544-03-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 165 In-stock
Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Solid
5 mg USD 96 In-stock
10 mg USD 150 In-stock
50 mg USD 220 In-stock
100 mg USD 380 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

GSTO1-IN-1 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

GSTO1-IN-1 is a potent glutathione S-transferase omega 1 (GSTO1) inhibitor with an IC50 of 31 nM.

IC50 & Target

IC50: 31 nM (GSTO1)[1]
In Vitro

GSTO1-IN-1 (C1-27) potently inhibits GSTO1 enzyme activity with an IC50 value of 31 nM. GSTO1-IN-1 also potently competes with 5-chloromethylfluorescein diacetate (CMFDA) for binding to recombinant protein, as well as endogenous GSTO1 in the milieu of a soluble proteome. HCT116 cells treated with GSTO1-IN-1 also show a decrease in cell viability in a dose-dependent manner. GSTO1-IN-1 inhibits the clonogenic survival of HCT116 cells at sub-micromolar concentrations[1].

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

GSTO1-IN-1 Related Antibodies
In Vivo

To test whether GSTO1-IN-1 had in vivo efficacy, its effects are evaluated in a human colon cancer cell line xenograft model. GSTO1-IN-1 (20-45 mg/kg) is administered as a single agent to nude mice bearing HCT116 xenografts. After 5 weeks of treatment, tumor growth is significantly inhibited in GSTO1-IN-1-treated mice compared with the vehicle-treated group (P<0.05). GSTO1-IN-1 treatment is generally well tolerated by mice up to 45 mg/kg, with no overt signs of toxicity and no significant variations in average body weights throughout the duration of the study[1].

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

311.18

Formula

C10H12Cl2N2O3S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC=C(Cl)C(S(=O)(N(C)C)=O)=C1)CCl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 300 mg/mL (964.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2136 mL 16.0679 mL 32.1357 mL
5 mM 0.6427 mL 3.2136 mL 6.4271 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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: ≥ 2.5 mg/mL (8.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Purity & Documentation
References
Cell Assay
[1]

Cell proliferation is assessed by a MTT assay. Cancer cells H630, HT29 and HCT116 are seeded in 96-well microtitre plates and, after overnight attachment, treated with GSTO1 inhibitors (e.g., GSTO1-IN-1; 0.1, 1, 10 and 100 μM). After 72 h, MTT solution (3 mg/mL; 20mL) is added to each well and cells are incubated for 3 h at 37°C. After incubation, media from each well is removed and the dark blue formazan crystals formed by live cells are dissolved in DMSO (150 mL per well). The absorbance intensity is measured at 570 nm on a microplate reader. Cell viability after 24 h treatment is assessed using ApoTox-Glo triplex assay. At least three independent dose-response experiments with each concentration tested in triplicate are performed for each cell line[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
In the pilot study, HCT116 cells (1×106) in exponential phase are injected subcutaneously into the left flank of 8- to 10-week-old female nude mice (25-30 g) . The perpendicular diameters of the tumors are measured three times weekly using standard calipers and tumour volumes are calculated. Tumors are allowed to grow to a volume of 50 mm3 and mice are randomized into control (n=5) and GSTO1-IN-1 (n=3) treatment groups. GSTO1-IN-1 is administered intraperitoneally (20 mg/kg per day) for the first 2 weeks on a 5 days on/2 days off schedule. The dose is then increased to 25 mg/kg per day for the next 23 days and further escalated by 5 mg/kg per day to a final dose of 45 mg/kg for the remaining duration of treatment. Tumor volumes and body weights are measured three times weekly to monitor tumor burden and weight loss during treatment. At the end of the experiment, animals are killed and tumor, kidney and liver are collected, fixed and paraffin embedded for histology[1].

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2136 mL 16.0679 mL 32.1357 mL 80.3394 mL
5 mM 0.6427 mL 3.2136 mL 6.4271 mL 16.0679 mL
10 mM 0.3214 mL 1.6068 mL 3.2136 mL 8.0339 mL
15 mM 0.2142 mL 1.0712 mL 2.1424 mL 5.3560 mL
20 mM 0.1607 mL 0.8034 mL 1.6068 mL 4.0170 mL
25 mM 0.1285 mL 0.6427 mL 1.2854 mL 3.2136 mL
30 mM 0.1071 mL 0.5356 mL 1.0712 mL 2.6780 mL
40 mM 0.0803 mL 0.4017 mL 0.8034 mL 2.0085 mL
50 mM 0.0643 mL 0.3214 mL 0.6427 mL 1.6068 mL
60 mM 0.0536 mL 0.2678 mL 0.5356 mL 1.3390 mL
80 mM 0.0402 mL 0.2008 mL 0.4017 mL 1.0042 mL
100 mM 0.0321 mL 0.1607 mL 0.3214 mL 0.8034 mL
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GSTO1-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSTO1-IN-1568544-03-6Glutathione S-transferaseGlutathione transferasesGSTsInhibitorinhibitorinhibit

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