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).

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.

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].

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).

CM121 is a reversible inhibitor of ALDH1A2 that acts specifically on the active site, exhibiting an IC50 of 0.54 μM and a Kd of 1.1 μM. It exerts its inhibitory effect through multiple hydrophobic interactions.

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].

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.

1. Aloenin (Aloenin A) and aloe-emodin are active principles for inhibition of c-ADH and c-ALDH activities in vitro.

Methyl diethyldithiocarbamate is an active metabolite of the aldehyde dehydrogenase inhibitor disulfiram .1It is produced by methylation of the disulfiram metabolite diethyldithiocarbamate in mouse liver microsomes.2Methyl diethyldithiocarbamate inhibits liver low Kmaldehyde dehydrogenase (ALDH) in rats (ID50= 15.5 mg/kg).1It decreases mean arterial pressure (MAP) and increases heart rate during ethanol challenge in rats when administered at a dose of 20.6 mg/kg. 1.Hart, B.W., Yourick, J.J., and Faiman, M.D.S-methyl-N,N-diethylthiolcarbamate: A disulfiram metabolite and potent rat liver mitochondrial low Km aldehyde dehydrogenase inhibitorAlcohol7(2)165-169(1990) 2.Gessner, T., and Jakubowski, M.Diethyldithiocarbamic acid methyl ester. A metabolite of disulfiramBiochem. Pharmacol.21(2)219-230(1972)

BODIPY-aminoacetaldehyde diethyl acetal (BAAA-DA) is a stable precursor to BODIPY-aminoacetaldehyde, a cell-permeable fluorescent substrate for aldehyde dehydrogenase (ALDH).1,2BODIPY-aminoacetaldehyde diethyl acetal is converted under acidic conditions to BODIPY-aminoacetaldehyde (BAAA).2BAAA is cell-permeant and is converted intracellularly by ALDH to BODIPY aminoacetate (BAA), which is retained by cells and can be used to identify cells with high ALDH activity.1BAA is a substrate for the efflux pump P-glycoprotein (P-gp) but co-application of BAAA with a P-gp inhibitor, such as verapamil , inhibits BAA efflux.2BAAA-DA has been used to isolate human hematopoietic progenitor cells, which have high ALDH activity, andviaflow cytometry to sort cancer stem cells that contain high levels of ALDH.1,3BAA used in cells can be excited at 488 nm and displays an emission maximum of 512 nm.4 1.Storms, R.W., Trujillo, A.P., Springer, J.B., et al.Isolation of primitive human hematopoietic progenitors on the basis of aldehyde dehydrogenase activityProceedings of the National Academy of Sciences of the United States of America96(16)9118-9123(1999) 2.Smith, C.A., Colvin, M., Storms, R.W., et al.BODIPY aminoacetaldehyde diethyl acetal08010501.81-15(2010) 3.Leng, Z., Yang, Z., Li, L., et al.A reliable method for the sorting and identification of ALDHhigh cancer stem cells by flow cytometryExp. Ther. Med.(2017) 4.Pomper, M.G., Wang, H., Minn, I., et al.Red fluorescent aldehyde dehydrogenase (ALDH) substrate(2015)

DOPAL is an aldehyde product of the oxidative deamination of dopamine by monoamine oxidase.[1] It can be further oxidized to 3,4-dihydroxyphenylacetic acid (DOPAC) by aldehyde dehydrogenase (ALDH) and, to a lesser extent reduced to 3,4-dihydroxyphenyl ethanol (DOPET). DOPAL is toxic to neurons.[2],[3] It can also oligomerize and precipitate α-synuclein, an event associated with Parkinson's disease.[2] Mice lacking cytosolic and mitochondrial forms of ALDH display increased levels of DOPAL as well as neurodegeneration and motor dysfunction characteristic of Parkinson's disease.[4]

ALDH3A1-IN-2 (Compound 19), a potent inhibitor of aldehyde dehydrogenases (ALDHs), demonstrates high efficacy against ALDH3A1 with an IC50 of 1.29 μM. Given the overexpression of ALDHs in multiple tumor types, including prostate cancer, ALDH3A1-IN-2 holds significant potential for cancer research [1].