Procainamide (hydrochloride) [614-39-1]
Referentie HY-A0084-1mL
Formaat : 10mM/1mL
Merk : MedChemExpress
| 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. |

