Aldehyde Dehydrogenase (ALDH) Inhibitor

ALDH1A3-IN-3 is a potent inhibitor of ALDH1A3, with an IC₅₀ of 0.26 μM. ALDH1A3-IN-3 is also a good ALDH3A1 substrate which limits its application as a selective inhibitor. ALDH1A3-IN-3 can be used for the research of prostate cancer.

CM010 is a potent and selective aldehyde dehydrogenase 1A (ALDH1A) family inhibitor, with IC₅₀s of 1700, 740, and 640 nM for ALDH1A1, ALDH1A2, and ALDH1A3, respectively. CM010 does not inhibit any of the other ALDH family members. CM010 can regulate metabolism and has anti-cancer activity.

EN40 is a potent, selective aldehyde dehydrogenase 3A1 (ALDH3A1) inhibitor as a covalent ligand, exhibits an IC₅₀ value of 2 uM

MCI-INI-3 is a selective ALDH1A3 inhibitor, with an IC₅₀ of 0.46 μM and a K_i of 0.55 μM against hALDH1A3. MCI-INI-3 inhibits retinoic acid (HY-14649) biosynthesis. MCI-INI-3 can be used in research related to glioblastoma and glioma.

KOTX1 is an orally active and selective ALDH1A3 inhibitor. KOTX1 improves glucose tolerance, insulin secretion and blood sugar levels in diabetic mouse models.

NCT-506 is an orally bioavailable aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with an IC₅₀ of 7 nM.

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.

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.

Hydrazine sulfate is an orally active PEPCK inhibitor. Hydrazine sulfate inhibits PEPCK and low-K_m ALDH. Hydrazine sulfate impairs gluconeogenesis and enhances the protective effect of energy substrates against MPP⁺ toxicity. Hydrazine sulfate exacerbates liver damage in rats when combined with Ethanol. Hydrazine sulfate can be used in the research of shock, non-small cell lung cancer, colorectal cancer and Parkinson's disease.

S-Methyl-N,N-diethylthiolcarbamate (DETC-Me; DDTC-Me) is the active metabolite of the aldehyde dehydrogenase inhibitor disulfiram (HY-B0240). It is produced by the methylation of the disulfiram metabolite diethyldithiocarbamate in mouse liver microsomes. S-Methyl-N,N-diethylthiolcarbamate (DETC-Me; DDTC-Me) inhibits rat liver low Km aldehyde dehydrogenase (ALDH) (ID50=15.5 mg/kg). When administered at a dose of 20.6 mg/kg, it decreases mean arterial pressure (MAP) and increases heart rate in rats during ethanol stimulation.

KS100 is a potent ALDH inhibitor with IC₅₀s of 230, 1542, 193 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS100 shows antiproliferative and anticancer effects with low low toxic. KS100 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS10600 induces apoptosis and cell cycle arrest at the G2/M phase.

4-Hydroxynonenal-d₃ is the deuterium labeled 4-Hydroxynonenal. 4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.

ALDH1A1-IN-2 (compound 297) is a potent inhibitor of aldehyde dehydrogenase 1a1 (aldh1a1). Aldehyde dehydrogenases (ALDH) constitute a family of enzymes that play a critical role in oxidizing various cytotoxic xenogenic and biogenic aldehydes. ALDH1A1-IN-2 has the potential for the research of cancer, inflammation, or obesity.

2-Bromoacetamide is a disinfection byproduct. 2-Bromoacetamide can inactivate liver alcohol dehydrogenase and interfere with microtubule and actin cytoskeletal function. 2-Bromoacetamide is a potent developmental toxicant in animals.

(6S)-CP-470711 (Compound 8) is an inhibitor for sorbitol dehydrogenase, that inhibits human and rat SDH with IC₅₀ of 19 nM and 27 nM. (6S)-CP-470711 ameliorates the Streptozotocin (HY-13753)-induced diabetes in rats models.

ALDH1A2-IN-1 is an active site-directed reversible ALDH1A2 inhibitor (IC₅₀=0.91 μM; Kd=0.26 μM) with several hydrophobic interactions.

Sorbitol dehydrogenase-IN-1 is a potent and orally active sorbitol dehydrogenase inhibitor with IC₅₀ s of 4, 5 nM for rat and human, respectively. Sorbitol Dehydrogenase (SDH) is an enzyme that belongs to the zinc-containing alcohol dehydrogenase (ADH) family. ADH and ALDH are enzymes that work together to metabolize alcohol.

Nitrefazole (EMD-15700) is an aldehyde dehydrogenase (ALDH) inhibitor. Nitrefazole specifically inhibits human liver ALDH I and human erythrocyte ALDH isozymes, but does not alter the activity of human liver ALDH II or human placental ALDH. Nitrefazole effectively promotes exosome secretion in prostate cancer cells by increasing the levels of Alix, nSMase2, Rab27a and p-ERK. Nitrefazole can be used in studies related to prostate cancer.

Daidzin (Standard) is the analytical standard of Daidzin. This product is intended for research and analytical applications. Daidzin is an isoflavone with antioxidant, anticancer, and antiatherosclerotic activities. Daidzin is a potent and selective inhibitor of mitochondrial ALDH-2. Daidzin reduces ethanol consumption.

NCT-505 is a potent and selective aldehyde dehydrogenase (ALDH1A1) inhibitor, with an IC₅₀ of 7 nM, and weakly inhibits hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 (IC₅₀s, >57, 22.8, 20.1, >57 μM).