aldh-1

Disulfiram (TETD) is an inhibitor of the acetaldehyde dehydrogenase ALDH, inhibiting hALDH1 and hALDH2 (IC50=0.15/1.45 μM) with specificity. Disulfiram is acutely sensitized to alcohol and also inhibits GSDMD pore formation.

4-Diethylaminobenzaldehyde, a reversible aldehyde dehydrogenase (ALDH) inhibitor (Ki: 4 nM for ALDH1), exhibits a potent anti-androgenic effect (IC50: 1.71 μM).

CM10 is an aldehyde dehydrogenase 1A family(ALDH1A) inhibitor.

ALDH1A3-IN-2 is a potent ALDH1A3 inhibitor with an IC50 of 0.30 μM.ALDH1A3-IN-2 has potential for cancer disease research.

α-NETA is a potent choline acetyltransferase (ChA) inhibitor and an ALDH1A1 and chemokine-like receptor 1 (CMKLR1) antagonist.Anti-cancer activity,Cholinesterase and acetylcholinesterase (AChE) inhibition,Dose-dependent reduction of body weight and fasting blood glucose levels in STZ-induced diabetic mice,Significantly reduced expression of renal injury markers,May be CEP-9722 can be used for the study of diabetic nephropathy.

inhibitor of aldehyde dehydrogenase 1a2 (ALDH1a2)

Daidzin (Daidzoside) is an isoflavone isolated from soya bean with anti-oxidant, anti-carcinogenic, and anti-atherosclerotic activities.

4-Isopropoxybenzaldehyde (compound 16), a powerful ALDH1A3 inhibitor with an IC50 of 0.26 μM (cell free assay), serves as an effective ALDH3A1 substrate. But shows weak antiproliferative effect against PC3, LNCaP, and DU145 PCa cell lines with IC50>200 μM[1].

CM037 (A-37) is a selective ALDH1A1 (acetaldehyde dehydrogenase 1A1) inhibitor (IC50; 4.6 µM) with antitumor activity and may be used in studies to eliminate gynecologic malignancies.

ALDH1A2-IN-1 is an active-site directed, reversible ALDH1A2 inhibitor that prevents spermatogenesis and can be used in male contraceptive research.

ALDH1A1-IN-4 (compound A1) functions as a powerful inhibitor of aldehyde dehydrogenase (ALDH) A1, exhibiting an IC 50 value of 0.32 μM. This compound is significant in cancer research [1].

NCT-505 is a potent and selective inhibitor of aldehyde dehydrogenase (ALDH1A1, IC50 = 7 nM) and a weak inhibitor of hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 with IC50 values of >57 μM, 22.8 μM, 20.1 μM, and >57 μM, respectively.

NR6 is an innovative and potent ALDH1A3 inhibitor with high selectivity. It effectively suppresses the growth of mesothelioma multicellular spheroids and the recruitment of neutrophils.

MCI-INI-3 is a selective competitive inhibitor of human ALDH1A3, with a Ki value of 0.55 μM for ALDH1A3 and 78.2 μM for ALDH1A1. It inhibits retinoic acid biosynthesis and can reduce the viability of glioblastoma cells GSC-83 and GSC-326.

ALDH1A1-IN-5 (compound 25) is a potent inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), exhibiting EC50 values of 83 µM, 45 µM, and 43 µM for ALDH1A1, ALDH1A2, and ALDH1A3, respectively. This compound holds potential for research in high-grade serous ovarian cancer (HGSOC).

CLM296 is a potent and selective inhibitor of ALDH1A3, with an IC50 of 2 nM. It does not exhibit off-target effects on the highly homologous ALDH1A1 isoform. CLM296 is capable of inhibiting ALDH1A3-driven breast cancer metastasis and can be utilized in the study of triple-negative breast cancer (TNBC).

NCT-501 hydrochloride is a highly potent and selective inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), which is based on theophylline. It effectively inhibits hALDH1A1 with an IC50 value of 40 nM, exhibiting superior selectivity towards hALDH1A1 compared to other ALDH isozymes and dehydrogenases such as hALDH1B1, hALDH3A1, and hALDH2 (with IC50 values exceeding 57 μM).

ALDH1A3-IN-1 (Compound 14) is a potent inhibitor of ALDH1A3, with IC50 = 0.63 μM and Ki = 0.46 μM, and is utilized in prostate cancer research [1].

KS106 is a selective and potent ALDH inhibitor with antiproliferative and anticancer activity, inhibits ALDH1A1, ALDH2, and ALDH3A1 with IC50 of 334, 2137, and 360 nM, respectively.KS106 contributes to apoptosis, induces an increase in G2/M cell cycle arrest, and can be used to study melanoma and colon cancer.

ALDH1A1-IN-2 is a potent aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitor with anticancer activity and may be used in research on breast cancer, inflammation, or obesity.

ALDH1A1-IN-3 is a good and selective inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1) (IC50: μM).ALDH1A1-IN-3 is effective in improving glucose consumption in HepG2 cells.ALDH1A1-IN-3 can be used for studies to improve glucose metabolism.

NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with an IC50 of 40 nM.

CM39 is an ALDH inhibitor. Aldehyde dehydrogenase (ALDH) activity is commonly used as a marker to identify cancer stem-like cells. The three ALDH1A isoforms have all been individually implicated in cancer stem-like cells and in chemoresistance.

CVT-10216 is a Potent and selective, reversible inhibitor of aldehyde dehydrogenase 2 (ALDH2) (IC50: 29 nM). CVT-10216 also has inhibitory effect of ALDH-1 (IC50: 1.3 μM). CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects.