KS106 is a potent ALDH inhibitor with IC50s of 334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS106 shows antiproliferative and anticancer effects with low low toxic.KS106 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS106 induces apoptosis and cell cycle arrest at the G2/M phase[1].
STL5-T-0057 (compound 68) is an selective ALDH1 B1 inhibitor with an IC50 value of 30 nM. STL5-T-0057 inhibits cell growth of SW480 cells in adherent and spheroid conditions with IC50 values of 2.46 and 0.39 μM, respectively. STL5-T-0057 can be used for the research of cancer[1].
Nitrefazole is a 4-nitroimidazole derivative with strong and long lasting inhibition of aldehyde dehydrogenase (ALDH), an enzyme involved in the metabolism of alcohol.
α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity[1][2].
ALDH1A3-IN-2 (Compound 15) is a potent inhibitor of ALDH1A3 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH1A3-IN-2 has the potential for the research of cancer diseases[1].
4-Diethylaminobenzaldehyde is a reversible aldehyde dehydrogenases (ALDHs) inhibitor, with a Ki of 4 nM for ALDH1. 4-Diethylaminobenzaldehyde displays potent anti-androgenic effect (IC50= 1.71μM)[1][2].
MeDTC (S-Methyl-N,N-diethylthiocarbamate Sulfone), a Disulfiram metabolite, is a potent, irreversible aldehyde dehydrogenase (ALDH) inhibitor[1].