2. Epigenetics Membrane Transporter/Ion Channel
  3. DNA Methyltransferase Potassium Channel
  4. Procainamide

Procainamide  (Synonyms: Procaine amide; SP 100)

Cat. No.: HY-A0084A Purity: 99.69%
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Procainamide (Procaine amide) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide relaxes airway smooth muscle by activating potassium channels. Procainamide can be used in cancer and arrhythmia research.

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

Procainamide Chemical Structure

Procainamide Chemical Structure

CAS No. : 51-06-9

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Based on 4 publication(s) in Google Scholar

Other Forms of Procainamide:

Procainamide Related Antibodies

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Description

Procainamide (Procaine amide) is a specific and potent inhibitor of DNA methyltransferase 1 (DNMT1), which reactivates the expression of tumor suppressor factors by demethylating tumor suppressor genes. Procainamide induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide relaxes airway smooth muscle by activating potassium channels. Procainamide can be used in cancer and arrhythmia research[1][2][3][4][5][6].

IC50 & Target

DNMT1[1]
In Vitro

Procainamide has a Ki of 7.2 μM for DNMT1 inhibition on hemimethylated oligonucleotide substrates and a Ki of 4600 μM for DNMT1 inhibition on unmethylated oligonucleotide substrates[1].
Procainamide (0.5 mM; 96 h) causes loss of CpG methylation in HCT116 cells and affects centromeric repeat sequences and single-copy genes[1].
Procainamide (0-10 mM) concentration-dependently relaxes bovine tracheal contractions induced by methacholine (0.3 μM) but does not significantly relax contractions induced by potassium ions (40 mM)[4].
Procainamide (250 μM-2.5 mM; 0-48 h) does not induce cellular vacuolization at a dose of 250 μM, but induces cellular vacuolization in many cells at a dose of 2.5 mM[5].
Procainamide (10 μM; 5 d) demethylates ER, p16, and RAR genes in MDA-231, T24, and MCF-7 cell lines[6].

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

Procainamide Related Antibodies
In Vivo

Procainamide (20 mg/kg; i.p.; once daily for 7 days) demethylates and re-expresses the ER gene in BALB/c mice xenografted with MDA-231 cells[6].

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

235.33

Formula

C13H21N3O
CAS No.
Appearance

Solid-Liquid Mixture

Color

White to light yellow

SMILES

O=C(NCCN(CC)CC)C1=CC=C(N)C=C1
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 : 50 mg/mL (212.47 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 4.2494 mL 21.2468 mL 42.4935 mL
5 mM 0.8499 mL 4.2494 mL 8.4987 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.

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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: ≥ 1.25 mg/mL (5.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (5.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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).

*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: 99.69%

COA (243 KB) HNMR (252 KB) LCMS (92 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 4.2494 mL 21.2468 mL 42.4935 mL 106.2338 mL
5 mM 0.8499 mL 4.2494 mL 8.4987 mL 21.2468 mL
10 mM 0.4249 mL 2.1247 mL 4.2494 mL 10.6234 mL
15 mM 0.2833 mL 1.4165 mL 2.8329 mL 7.0823 mL
20 mM 0.2125 mL 1.0623 mL 2.1247 mL 5.3117 mL
25 mM 0.1700 mL 0.8499 mL 1.6997 mL 4.2494 mL
30 mM 0.1416 mL 0.7082 mL 1.4165 mL 3.5411 mL
40 mM 0.1062 mL 0.5312 mL 1.0623 mL 2.6558 mL
50 mM 0.0850 mL 0.4249 mL 0.8499 mL 2.1247 mL
60 mM 0.0708 mL 0.3541 mL 0.7082 mL 1.7706 mL
80 mM 0.0531 mL 0.2656 mL 0.5312 mL 1.3279 mL
100 mM 0.0425 mL 0.2125 mL 0.4249 mL 1.0623 mL
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Procainamide 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:

Procainamide51-06-9Procaine amide SP 100SP100SP 100SP-100DNA MethyltransferasePotassium ChannelDNMTsDNA MTasesKcsADNA methyltransferase 1DNMT1Class 1AantiarrhythmiccancerarrhythmiasInhibitorinhibitorinhibit

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