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

Procainamide hydrochloride  (Synonyms: Procaine amide hydrochloride; SP 100 hydrochloride)

Cat. No.: HY-A0084 Purity: ≥98.0%
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Procainamide hydrochloride (Procaine amide hydrochloride) 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 hydrochloride induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide hydrochloride relaxes airway smooth muscle by activating potassium channels. Procainamide hydrochloride can be used in cancer and arrhythmia research.

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

Procainamide hydrochloride Chemical Structure

Procainamide hydrochloride Chemical Structure

CAS No. : 614-39-1

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Based on 4 publication(s) in Google Scholar

Other Forms of Procainamide hydrochloride:

Procainamide hydrochloride Related Antibodies

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Description

Procainamide hydrochloride (Procaine amide hydrochloride) 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 hydrochloride induces vacuolization in various cell types and reduces cell proliferation and migration. Procainamide hydrochloride relaxes airway smooth muscle by activating potassium channels. Procainamide hydrochloride can be used in cancer and arrhythmia research[1][2][3][4][5][6].

IC50 & Target

DNMT1[1]
In Vitro

Procainamide hydrochloride 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 hydrochloride (0.5 mM; 96 h) causes loss of CpG methylation in HCT116 cells and affects centromeric repeat sequences and single-copy genes[1].
Procainamide hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride Related Antibodies
In Vivo

Procainamide hydrochloride (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

271.79

Formula

C13H22ClN3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCCN(CC)CC)C1=CC=C(N)C=C1.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (183.97 mM)

DMSO : 50 mg/mL (183.97 mM; Need ultrasonic; 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 3.6793 mL 18.3966 mL 36.7931 mL
5 mM 0.7359 mL 3.6793 mL 7.3586 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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: ≥ 3.25 mg/mL (11.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 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: ≥ 3.25 mg/mL (11.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 120 mg/mL (441.52 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation
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 (sealed storage, away from moisture and 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
H2O / DMSO 1 mM 3.6793 mL 18.3966 mL 36.7931 mL 91.9828 mL
5 mM 0.7359 mL 3.6793 mL 7.3586 mL 18.3966 mL
10 mM 0.3679 mL 1.8397 mL 3.6793 mL 9.1983 mL
15 mM 0.2453 mL 1.2264 mL 2.4529 mL 6.1322 mL
20 mM 0.1840 mL 0.9198 mL 1.8397 mL 4.5991 mL
25 mM 0.1472 mL 0.7359 mL 1.4717 mL 3.6793 mL
30 mM 0.1226 mL 0.6132 mL 1.2264 mL 3.0661 mL
40 mM 0.0920 mL 0.4599 mL 0.9198 mL 2.2996 mL
50 mM 0.0736 mL 0.3679 mL 0.7359 mL 1.8397 mL
60 mM 0.0613 mL 0.3066 mL 0.6132 mL 1.5330 mL
80 mM 0.0460 mL 0.2300 mL 0.4599 mL 1.1498 mL
100 mM 0.0368 mL 0.1840 mL 0.3679 mL 0.9198 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Procainamide hydrochloride 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:

Procainamide614-39-1Procaine amideSP 100SP100SP-100DNA MethyltransferasePotassium ChannelDNMTsDNA MTasesKcsADNA methyltransferase 1DNMT1Class 1AantiarrhythmiccancerarrhythmiasInhibitorinhibitorinhibit

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