2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. TMS

TMS  (Synonyms: (E)-2,3',4,5'-tetramethoxystilbene)

Cat. No.: HY-19340 Purity: 98.61%
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TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive CYP1B1 inhibitor with an IC50 of 6 nM and a Ki value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC50=300 nM) and CYP1A2 (IC50=3.1 μM). TMS is a methylated derivative of resveratrol and has anti-cancer activity.

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

TMS Chemical Structure

TMS Chemical Structure

CAS No. : 24144-92-1

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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 66 In-stock
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Based on 6 publication(s) in Google Scholar

TMS Related Antibodies

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive CYP1B1 inhibitor with an IC50 of 6 nM and a Ki value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC50=300 nM) and CYP1A2 (IC50=3.1 μM). TMS is a methylated derivative of resveratrol and has anti-cancer activity[1][2][3].

IC50 & Target[1]

CYP1B1

6 nM (IC50)

CYP1B1

3 nM (Ki)

CYP1A1

300 nM (IC50)

CYP1A2

3.1 μM (IC50)

In Vitro

TMS, an analogue of resveratrol, is considered to be a potential cancer preventive agent since it is a potent inhibitor of CYP1B1. To assess survival of MCF-7 cells exposed to 1 μM benzo[a]pyrene (BP), 1 μM BP+1 μM TMS and 1 μM BP+4 μM TMS, cells ae incubated for up to 72 h without a media change. Luminescence units from exposed cells, expressed as a percentage of luminescence units from solvent (DMSO)-treated cells at the same time intervals. In all exposure groups, cell viability remains >90% for the first 24 h, but by 72 h, cell survival drops to 60-70%[1].

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

TMS Related Antibodies
In Vivo

To determine the contribution of CYP1B1 in development of hypertension in spontaneously hypertensive rats (SHR), the effect of TMS is examined on in SHR and WKY rats. Systolic BP steadily increases in SHR from 4 weeks of age. Starting from 8 weeks of age, daily injections of TMS reduce systolic BP in SHR to levels observed at the beginning of the experiment (207±7 vs. 129±2 mmHg). Systolic BP is not altered in WKY injected with TMS or its vehicle (129±7 vs. 127±4 mmHg) [1].

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

300.35

Formula

C18H20O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

COC1=CC=C(/C=C/C2=CC(OC)=CC(OC)=C2)C(OC)=C1
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 : ≥ 50 mg/mL (166.47 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 3.3294 mL 16.6472 mL 33.2945 mL
5 mM 0.6659 mL 3.3294 mL 6.6589 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.

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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 (8.32 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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 viability is determined using the Cell Titer Glo Luminescent Cell Viability Assay. In brief, MCF-7 cells are seeded in 12-well plates (75 000 cells per well) in triplicate. Attached cells are exposed to 1 μM BP in the presence of 0, 1 or 4 μM TMS. At 4, 12, 24 or 72 h, RIPA Lysis Buffer (1x) is added to lyse the cells. A diluted sample of homogeneous cell lysate is transferred in duplicate to a 96-well plate and combined with an equivalent volume of Cell Titer Glo Luminescence. Luminescence measure using the Tropix 717 Microplate Luminometer. To examine viability of cells exposed to BP alone, the 72-h treatment is repeated twice, and for each experiment cells are assayed in triplicate. The values are expressed as % of the DMSO-alone solvent control[1].

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

Mice[1]
36 three-weeks-old male spontaneously hypertensive rats (SHR) and 36 age-matched WKY are used throughout this research. Each strain of rats is split into two groups; one group is injected daily with TMS (600 μg/kg) and the other with vehicle (DMSO; 100 μL) beginning at 8 weeks of age. Systolic BP and mean arterial pressure (MAP) are measured twice a week from 4 weeks of age; a noninvasive tail cuff method is used[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 3.3294 mL 16.6472 mL 33.2945 mL 83.2362 mL
5 mM 0.6659 mL 3.3294 mL 6.6589 mL 16.6472 mL
10 mM 0.3329 mL 1.6647 mL 3.3294 mL 8.3236 mL
15 mM 0.2220 mL 1.1098 mL 2.2196 mL 5.5491 mL
20 mM 0.1665 mL 0.8324 mL 1.6647 mL 4.1618 mL
25 mM 0.1332 mL 0.6659 mL 1.3318 mL 3.3294 mL
30 mM 0.1110 mL 0.5549 mL 1.1098 mL 2.7745 mL
40 mM 0.0832 mL 0.4162 mL 0.8324 mL 2.0809 mL
50 mM 0.0666 mL 0.3329 mL 0.6659 mL 1.6647 mL
60 mM 0.0555 mL 0.2775 mL 0.5549 mL 1.3873 mL
80 mM 0.0416 mL 0.2081 mL 0.4162 mL 1.0405 mL
100 mM 0.0333 mL 0.1665 mL 0.3329 mL 0.8324 mL
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TMS 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:

TMS24144-92-1(E)-2,3',4,5'-tetramethoxystilbeneCytochrome P450CYPsInhibitorinhibitorinhibit

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