Cat. No.: HY-A0084A

Procainamide

(Synonyms: Procaine amide; SP 100)

7 Cited Publications

Customer Review

Based on 7 publication(s) in Google Scholar

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.

Purity: 99.80%
CAS No.: 51-06-9
Formula: C₁₃H₂₁N₃O
Molecular Weight:235.33

Storage:

4°C, protect from light

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

Procainamide Chemical Structure

CAS No.: 51-06-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (7)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

DNMT1^[1]

All DNA Methyltransferase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	389.5 μM Compound: procainamide	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
HEK293	IC₅₀	12 μM Compound: Procainamide	TP_TRANSPORTER: inhibition of TEA uptake (in the absence of bicarbonate) (TEA: 20 uM) in OCT1-expressing HEK293 cells TP_TRANSPORTER: inhibition of TEA uptake (in the absence of bicarbonate) (TEA: 20 uM) in OCT1-expressing HEK293 cells	[PMID: 12438515]
HEK293	IC₅₀	215 μM Compound: Procainamide	TP_TRANSPORTER: inhibition of TEA uptake (in the absence of bicarbonate) (TEA: 20 uM) in OCT2-expressing HEK293 cells TP_TRANSPORTER: inhibition of TEA uptake (in the absence of bicarbonate) (TEA: 20 uM) in OCT2-expressing HEK293 cells	[PMID: 12438515]
HEK293	IC₅₀	7 μM Compound: Procainamide	TP_TRANSPORTER: inhibition of TEA uptake (in the presence of bicarbonate) (TEA: 20 uM) in OCT1-expressing HEK293 cells TP_TRANSPORTER: inhibition of TEA uptake (in the presence of bicarbonate) (TEA: 20 uM) in OCT1-expressing HEK293 cells	[PMID: 12438515]
HEK293	IC₅₀	90 μM Compound: Procainamide	TP_TRANSPORTER: inhibition of TEA uptake (in the presence of bicarbonate) (TEA: 20 uM) in OCT2-expressing HEK293 cells TP_TRANSPORTER: inhibition of TEA uptake (in the presence of bicarbonate) (TEA: 20 uM) in OCT2-expressing HEK293 cells	[PMID: 12438515]
HRPE	IC₅₀	1 mM Compound: Procainamide	TP_TRANSPORTER: inhibition of TEA uptake in Octn1-HRPE cells TP_TRANSPORTER: inhibition of TEA uptake in Octn1-HRPE cells	[PMID: 10825452]
Oocyte	IC₅₀	445 μM Compound: Procainamide	TP_TRANSPORTER: inhibition of TEA uptake (TEA: 10 uM) in Xenopus laevis oocytes TP_TRANSPORTER: inhibition of TEA uptake (TEA: 10 uM) in Xenopus laevis oocytes	[PMID: 11502595]
Oocyte	IC₅₀	167 μM Compound: Procainamide	TP_TRANSPORTER: inhibition pramipexole uptake in rOCT2-injected oocytes TP_TRANSPORTER: inhibition pramipexole uptake in rOCT2-injected oocytes	[PMID: 15640376]
Oocyte	IC₅₀	7.7 μM Compound: Procainamide	TP_TRANSPORTER: inhibition pramipexole uptake in rOCT1-injected oocytes TP_TRANSPORTER: inhibition pramipexole uptake in rOCT1-injected oocytes	[PMID: 15640376]
Sf9	IC₅₀	>300 μM Compound: 8	Inhibition of His6-tagged human recombinant DNMT3A/DNMT3L expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid Inhibition of His6-tagged human recombinant DNMT3A/DNMT3L expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid	[PMID: 25406944]
Sf9	IC₅₀	>500 μM Compound: 8	Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintil Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintil	[PMID: 25406944]

In Vitro

Procainamide has a K_i of 7.2 μM for DNMT1 inhibition on hemimethylated oligonucleotide substrates and a K_i 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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 51-06-9
Appearance <47°C Solid,>47°C Liquid
Molecular Weight 235.33
Formula C₁₃H₂₁N₃O
Color White to light yellow
SMILES

O=C(NCCN(CC)CC)C1=CC=C(N)C=C1
Synonyms

Procaine amide; SP 100
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)

Publications (7)

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Journal Impact Factor

Adv Sci (Weinh)

Targeted SPP1 Inhibition of Tumor-Associated Myeloid Cells Effectively Decreases Tumor Sizes. [Abstract]

2025 Jan;12(4):e2410360. PMID: 39639496
Clin Chem

Discovering Cross-Reactivity in Urine Drug Screening Immunoassays through Large-Scale Analysis of Electronic Health Records. [Abstract]

2019 Dec;65(12):1522-1531. PMID: 31578215
Free Radic Biol Med

Cannabidiol mitigates radiation-induced intestine ferroptosis via facilitating the heterodimerization of RUNX3 with CBFβ thereby promoting transactivation of GPX4. [Abstract]

2024 Sep:222:288-303. PMID: 38830513
Environ Pollut

Investigating the role and mechanism of methionine in different types of skeletal fluorosis based on Siglec-15 methylation. [Abstract]

2026 Feb 1:390:127432. PMID: 41349947
Environ Pollut

Screening of differentially methylated genes in skeletal fluorosis of rats with different types and involvement of aberrant methylation of Cthrc1. [Abstract]

2023 Sep 1:332:121931. PMID: 37268221
Drug Metab Dispos

An in vitro approach to predict idiosyncratic drug-induced agranulocytosis using myeloperoxidase-derived reactive metabolites. [Abstract]

2026 Jun;54(6):100324. PMID: 42248123
Patent

US20180263995A1.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.2494 mL

21.2468 mL

42.4935 mL

5 mM

0.8499 mL

4.2494 mL

8.4987 mL

10 mM

0.4249 mL

2.1247 mL

4.2494 mL

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

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

Mass Mass

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Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 1.25 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 (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Lee BH, et al. Procainamide is a specific inhibitor of DNA methyltransferase 1. J Biol Chem. 2005;280(49):40749-40756. [Content Brief]

[2]. Pritchard B, et al. Procainamide. [Updated 2021 Aug 8]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2022 Jan-.

[3]. Gardner I, et al. A comparison of the covalent binding of clozapine, procainamide, and vesnarinone to human neutrophils in vitro and rat tissues in vitro and in vivo[J]. Chemical research in toxicology, 2005, 18(9): 1384-1394. [Content Brief]

[4]. Nakahara T, et al. Involvement of K+ channel in procainamide-induced relaxation of bovine tracheal smooth muscle[J]. European journal of pharmacology, 2000, 402(1-2): 143-149. [Content Brief]

[5]. Morissette G, et al. Massive cell vacuolization induced by organic amines such as procainamide[J]. Journal of Pharmacology and Experimental Therapeutics, 2004, 310(1): 395-406. [Content Brief]

[6]. Segura-Pacheco B, et al. Reactivation of tumor suppressor genes by the cardiovascular drugs hydralazine and procainamide and their potential use in cancer therapy[J]. Clinical Cancer Research, 2003, 9(5): 1596-1603. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Publications Citing Use of MedChemExpress (MCE) Procainamide

All DNA Methyltransferase Isoforms

Biological Activity

Chemical Information

Publications (7)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Procainamide Related Classifications

HY-A0084A Related Classifications