Aldehyde Dehydrogenase (ALDH)

ALDH1A1-IN-3 is a selective inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), demonstrating an IC50 value of 0.379 μM. This compound effectively enhances glucose consumption in HepG2 cells, making it a valuable tool for studying glucose metabolism. ALDH1A1-IN-3 is suitable for research applications focused on metabolic regulation and potential therapeutic interventions in metabolic disorders.

Aldi-2 is a selective covalent inhibitor of aldehyde dehydrogenases (ALDHs), exhibiting IC50 values of 2.5, 6.4, and 1.9 μM for ALDH1A1, ALDH2, and ALDH3A1, respectively. This compound is particularly valuable in cancer research, providing insight into the role of ALDHs in tumor metabolism and progression. Its specificity allows for targeted studies on the modulation of ALDH activity within various biological contexts.

CM026 is a selective inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), demonstrating submicromolar potency. The compound exerts its inhibitory effect through binding to the aldehyde binding pocket, specifically involving a unique glycine residue. CM026 serves as a valuable chemical tool for investigating the role of ALDH1A1 in various pathological conditions and studying its implications in disease research.

ALDH2 Modulator 1 is a potent modulator of aldehyde dehydrogenase-2 (ALDH2), showcasing effective oral bioavailability. This compound has been demonstrated to significantly reduce blood alcohol levels in murine models, highlighting its potential applications in alcohol metabolism research and related metabolic studies.

ALDH3A1-IN-4 is a selective inhibitor of ALDH3A1, exhibiting an IC50 of 0.2 μM. This compound interacts with the aldehyde-binding pocket of ALDH3A1 through hydrophobic interactions and van der Waals forces. ALDH3A1-IN-4 functions as a chemosensitizer, enhancing the antiproliferative effects of mafosfamide in ALDH3A1-expressing cancer cells while sparing non-cancer cells. It is particularly relevant for research on lung adenocarcinoma and glioblastoma.

NCT-501 hydrochloride is a highly potent and selective inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), demonstrating an IC50 of 40 nM. It exhibits superior selectivity against other ALDH isozymes, as well as various dehydrogenases, with IC50 values greater than 57 μM for hALDH1B1, hALDH3A1, and hALDH2. This compound is valuable for research applications focused on cancer biology, neurodegenerative diseases, and other conditions where ALDH1A1 activity plays a critical role.

ALDH3A1-IN-2 is a potent inhibitor of aldehyde dehydrogenase 3A1 (ALDH3A1) with an IC50 of 1.29 μM. This compound is particularly relevant for research in oncology, as ALDHs, including ALDH3A1, are often overexpressed in various tumor types, such as prostate cancer. ALDH3A1-IN-2 may provide valuable insights into the role of ALDH3A1 in cancer progression and therapeutic intervention.

GA11 is an inhibitor of aldehyde dehydrogenase (ALDH), demonstrating significant anti-glioblastoma activity in both in vitro and in vivo models. This compound is valuable for research applications focusing on cancer biology and therapeutic strategies targeting glioblastoma through ALDH modulation.

ALDH1A1 modulator-1 is a selective modulator of the aldehyde dehydrogenase 1A1 (ALDH1A1) enzyme. This compound exhibits the ability to influence ALDH1A1 activity, which plays a critical role in the detoxification of aldehydes and the metabolic regulation of retinoic acid. ALDH1A1 modulator-1 is valuable for research focused on cancer biology, stem cell differentiation, and metabolic disorders, providing insights into the modulation of ALDH1A1 in various biological contexts.

CM-39 is a non-covalent, reversible inhibitor of aldehyde dehydrogenase 1A (ALDH1A), exhibiting an IC50 of 0.9 μM. This compound is used in research applications focusing on the modulation of cellular aldehyde metabolism and the study of cancer biology, where ALDH1A plays a significant role in stem cell regulation and chemoresistance. It provides a valuable tool for scientists investigating the therapeutic potential of targeting ALDH pathways in various disease models.

PKM2-IN-7 is a selective inhibitor of pyruvate kinase M2 (PKM2) that disrupts the interaction between PKM2 and ALDH1A3, demonstrating minimal toxicity to normal cells. This compound is pivotal for investigations into tumor biology, making it an essential tool for research focused on cancer metabolism and tumorigenesis.

Nitrofen is a selective contact herbicide that functions as an inhibitor of retinal dehydrogenase, a member of the aldehyde dehydrogenase (ALDH) family, as well as protoporphyrinogen oxidase. Its primary mechanism involves disrupting the biosynthetic pathways of chlorophyll, leading to effective weed control. Nitrofen is commonly utilized in agricultural research to investigate herbicidal activities and the underlying biochemical mechanisms of herbicide resistance.

D-6-Oxo-pipecolinic acid is the D-enantiomer of 6-Oxo-pipecolinic acid and serves as a biomarker for pyridoxine-dependent epilepsy (PDE) linked to the ALDH7A1 gene. This compound is crucial for studying the metabolic pathways associated with PDE, facilitating research into neurological disorders and potential therapeutic interventions. Its role as a biomarker allows for better understanding and diagnosis of pyridoxine-dependent epilepsy.

Iodoquine is a chloroquine analog that primarily targets cancer cells. It demonstrates significant uptake in tumor cells, particularly in those with elevated ALDH1 content, such as cancer stem cells, while exhibiting minimal accumulation in normal brain tissue. This unique profile makes iodoquine a valuable tool for research applications related to tumor diagnosis and as a radiotracer in cancer studies.

Crocetin dialdehyde is a non-volatile apocarotenoid derived from the enzymatic activity of CCD2 on zeaxanthin in saffron. This compound exhibits potential biological activity and can be metabolized by aldehyde dehydrogenases (ALDHs) to form crocetin. Research applications include studies on carotenoid metabolism and exploring its effects on cellular and physiological processes. Notably, crocetin dialdehyde has been observed to have no detrimental effects on liver function in murine models.

BODIPY aminoacetaldehyde diethyl acetal is a stable precursor to BODIPY-aminoacetaldehyde, which serves as a fluorescent substrate for aldehyde dehydrogenase (ALDH). Under acidic conditions, it can be efficiently converted into BODIPY-aminoacetaldehyde, facilitating studies of ALDH activity and function. This reagent is valuable for applications in fluorescence microscopy, biochemical assays, and other research areas focused on enzymatic activity and metabolic pathways.

Sulfiram is an ectoparasiticide that functions primarily as a weak inhibitor of aldehyde dehydrogenase (ALDH). It is utilized in the investigation of scabies, providing a valuable tool for understanding the biochemical pathways involved in ectoparasitic infections. Additionally, Sulfiram's inhibitory properties make it relevant for research exploring ALDH-related metabolic processes.

Camelliquercetiside D is a natural product that acts as an alcohol dehydrogenase inhibitor, demonstrating an IC50 of 41.5 μM against yeast ADH. This compound is isolated from the leaves of Camellia sinensis and exhibits notable scavenging activity against DPPH, making it valuable for research applications in enzymology and oxidative stress studies.

Camelliquercetiside B is a natural product that serves as an alcohol dehydrogenase inhibitor. Isolated from the leaves of Camellia sinensis, it demonstrates significant inhibitory activity with an IC50 value of 13.7 μM against yeast alcohol dehydrogenase. In addition, Camelliquercetiside B displays scavenging activity against DPPH free radicals, making it a valuable tool for research in alcohol metabolism and oxidative stress studies.