2. Apoptosis Epigenetics
  3. Apoptosis Histone Demethylase MDM-2/p53
  4. Methylstat

Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis.

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Methylstat Chemical Structure

Methylstat Chemical Structure

CAS No. : 1310877-95-2

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Based on 1 publication(s) in Google Scholar

Methylstat Related Antibodies

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1 Publications Citing Use of MCE Methylstat

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  • Biological Activity

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Description

Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis[1][2].

Cellular Effect
Cell Line Type Value Description References
KYSE-150 cell line GI50
5.1 μM
Compound: 216
Growth inhibition of human KYSE-150 cells after 48 hrs
Growth inhibition of human KYSE-150 cells after 48 hrs
10.1039/C1MD00199J
KYSE-150 cell line GI50
5.1 μM
Compound: 4b
Growth inhibition of human KYSE-150 cells measured after 48 hrs
Growth inhibition of human KYSE-150 cells measured after 48 hrs
[PMID: 35838529]
In Vitro

Methylstat (0-5 μM; 48, 72 h) shows anti-proliferative activity with no cytotoxicity on HUVECs at 1-2 μM[1].
Methylstat (0, 1, 2 μM; 48 h) induces cell cycle arrest at G0/G1 phase in a dose-dependent manner[1].
Methylstat (0, 1, 2 μM; 48 h) increases the expression of p53 mRNA levels, the H3K27 methylation levels and the accumulation of p53 and p21 protein levels, but suppresses the protein level of cyclinD1[1].
Methylstat (0, 1, 2 μM) shows anti-angiogenic activity induced by VEGF, bFGF and TNF-α in HUVEC cells, and inhibits the f capillary formation during CAM (chick embryo chorioallantoic membrane) development without any sign of thrombosis and hemorrhage[1].
Methylstat (1.1, 2.2 mM for U266 cells, 2.1, 4.2 mM for ARH77 cells; 72 h) induces apoptosis significantly in U266 and ARH77 cells[2].

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

Methylstat Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HUVEC cells
Concentration: 0-5 µM
Incubation Time: 48, 72 h
Result: Did not exhibit cytotoxicity on HUVECs at 1-2 µM.

Cell Viability Assay[1]

Cell Line: HUVEC, HepG2, HeLa, CHANG cells
Concentration: 0-5 µM
Incubation Time: 72 h
Result: Showed anti-proliferative activity with IC50s of 4, 10, 5, 7.5 µM for HUVEC, HepG2, HeLa, CHANG cells, respectively.

Cell Cycle Analysis[1]

Cell Line: HUVEC cells
Concentration: 0, 1, 2 µM
Incubation Time: 48 h
Result: G0/G1 phase increased 16.8% compared to non-treated cells, whereas S and G2/M decreased 5.5% and 6.1% respectively.

Western Blot Analysis[1]

Cell Line: HUVEC cells
Concentration: 0, 1, 2 µM
Incubation Time: 0-48 h
Result: Resulted in accumulation of p53 and p21 protein levels in a time- and dose-dependent manner and increased the H3K27 methylation levels, the but suppressed the protein level of cyclinD1.

Apoptosis Analysis[2]

Cell Line: U266, ARH77 cells
Concentration: 1.1, 2.2 mM for U266 cells, 2.1, 4.2 mM for ARH77 cells
Incubation Time: 72 h
Result: Induced apoptosis in U266, ARH77 cells.
Molecular Weight

505.56

Formula

C28H31N3O6
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

COC(/C=C/C(N(O)CCCCNCC(C=C1)=CC=C1COC(NC2=CC=CC3=C2C=CC=C3)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (197.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9780 mL 9.8900 mL 19.7800 mL
5 mM 0.3956 mL 1.9780 mL 3.9560 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (4.95 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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Dosing volume
(per animal)

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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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

Purity: 98.34%

SDS (252 KB)

COA (242 KB) HNMR (286 KB) LCMS (263 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month (protect from light). 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 1.9780 mL 9.8900 mL 19.7800 mL 49.4501 mL
5 mM 0.3956 mL 1.9780 mL 3.9560 mL 9.8900 mL
10 mM 0.1978 mL 0.9890 mL 1.9780 mL 4.9450 mL
15 mM 0.1319 mL 0.6593 mL 1.3187 mL 3.2967 mL
20 mM 0.0989 mL 0.4945 mL 0.9890 mL 2.4725 mL
25 mM 0.0791 mL 0.3956 mL 0.7912 mL 1.9780 mL
30 mM 0.0659 mL 0.3297 mL 0.6593 mL 1.6483 mL
40 mM 0.0495 mL 0.2473 mL 0.4945 mL 1.2363 mL
50 mM 0.0396 mL 0.1978 mL 0.3956 mL 0.9890 mL
60 mM 0.0330 mL 0.1648 mL 0.3297 mL 0.8242 mL
80 mM 0.0247 mL 0.1236 mL 0.2473 mL 0.6181 mL
100 mM 0.0198 mL 0.0989 mL 0.1978 mL 0.4945 mL
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Methylstat 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:

Methylstat1310877-95-2ApoptosisHistone DemethylaseMDM-2/p53anti-proliferativelow cytotoxicityG0/G1 phasep53apoptosisHUVECsanti-angiogenicInhibitorinhibitorinhibit

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