Aldehyde Dehydrogenase (ALDH)

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.

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.

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

Propachlor is a specific ALDH1A1 inhibitor. It is sometimes used as an herbicide.

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

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).

RV01 is an analogue of resveratrol, inhibits DNA damage, reduces acetaldehyde dehydrogenase 2 (ALDH2) mRNA expression induced by ethanol, and exhibits hydroxyl radical scavenging activity. RV01 decreases iNOS expression, with anti-neuroinflammatory activity.

KS106 is a selective inhibitor of aldehyde dehydrogenase (ALDH), demonstrating IC50 values of 334 nM for ALDH1A1, 2137 nM for ALDH2, and 360 nM for ALDH3A1. This compound exhibits significant antiproliferative and anticancer properties while maintaining low toxicity. KS106 effectively increases reactive oxygen species (ROS) levels, enhances lipid peroxidation, and leads to the accumulation of toxic aldehydes. Furthermore, it promotes apoptosis and induces cell cycle arrest at the G2/M phase, making it a valuable tool for cancer research and therapeutic studies.

KS100 is a potent inhibitor of aldehyde dehydrogenase (ALDH), demonstrating IC50 values of 230 nM for ALDH1A1, 1542 nM for ALDH2, and 193 nM for ALDH3A1. This compound exhibits significant antiproliferative and anticancer effects with minimal toxicity. KS100's mechanism includes the induction of reactive oxygen species (ROS), lipid peroxidation, and accumulation of toxic aldehydes. Additionally, it triggers apoptosis and causes cell cycle arrest at the G2/M phase, making it a valuable tool for cancer research.

AD-9308 is a selective and orally active activator of aldehyde dehydrogenase 2 (ALDH2), enhancing the clearance of 4-Hydroxy-2-nonenal (4-HNE) and thereby reducing myocardial fibrosis, inflammation, and apoptosis. It improves mitochondrial function and sarcoplasmic reticulum calcium transport, while also regulating autophagy to restore intracellular homeostasis. In experimental models of diabetes, AD-9308 has demonstrated the ability to enhance both diastolic and systolic heart function, as well as reverse ventricular remodeling. This compound serves as a valuable tool for studying diabetic cardiomyopathy and related cardiac disorders.

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.