Aldehyde Dehydrogenase (ALDH)

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  1. ALDH2 Activator

    Alda 1 is an activator of aldehyde dehydrogenase 2 (ALDH2).
  2. hALDH1 Inhibitor

    NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with IC50 of 40 nM.
  3. ALDH2 inhibitor

    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.
  4. ALDH1A1 inhibitors

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

    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).
  6. ALDH1A1 inhibitor

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

    Trans-3-Indoleacrylic acid is a ferroptosis inhibitor that acts through modulation of the AHR-ALDH1A3-FSP1-CoQ10 axis. It has been shown to promote tumor development by inhibiting RSL3-induced ferroptosis, thereby contributing to the progression of colorectal carcinogenesis. This compound serves as a valuable tool for research into ferroptosis mechanisms and cancer biology.
  8. ALDH Inhibitor/Local Anaesthetic

    Dyclonine hydrochloride is a potent inhibitor of aldehyde dehydrogenases (ALDH), specifically targeting ALDH2 with an IC50 of 35 μM and ALDH3A1 with an IC50 of 76 μM. This compound exhibits notable biological activities, including the sensitization of targeted cancer cells and antibacterial properties. Additionally, Dyclonine hydrochloride serves as a local anesthetic, effectively inhibiting nerve impulse transmission and alleviating pain sensations. Its ability to cross the blood-brain barrier further enhances its utility in various research applications.
  9. ChA Inhibitor

    α-NETA is a potent noncompetitive inhibitor of choline acetyltransferase (ChA), exhibiting an IC50 value of 9 μM. Additionally, it displays strong antagonistic activity against aldehyde dehydrogenase 1A1 (ALDH1A1) with an IC50 of 0.04 µM and also targets chemokine-like receptor-1 (CMKLR1). While it shows some inhibitory effects on cholinesterase (ChE) and acetylcholinesterase (AChE) with higher IC50 values, α-NETA is notable for its anti-cancer properties, making it a valuable tool for research in cancer biology and neuropharmacology.
  10. ALDH Inhibitor

    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.
  11. ALDH Inhibitor

    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.
  12. ALDH2 Activator

    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.
  13. Substrate For ALDH, Precursor Compound for Phenolic Compounds

    3-Hydroxybenzaldehyde serves as a substrate for aldehyde dehydrogenase (ALDH) and acts as a precursor for diverse phenolic compounds, including Protocatechuic aldehyde. This compound exhibits vasculoprotective properties, demonstrating potential in both in vitro and in vivo studies. Research applications primarily focus on its role in atherosclerosis, making it a valuable reagent for biochemical investigations related to cardiovascular health.
  14. SMO Inhibitor

    IPI-269609 is a potent inhibitor of Smoothened (SMO), specifically targeting the Hedgehog (Hh) signaling pathway. This compound has demonstrated significant efficacy in reducing the ALDH-bright cell population, identified as cancer stem cells in pancreatic cancer. IPI-269609 effectively inhibits both the migration and colony formation of pancreatic cancer cells, and has shown effectiveness in mitigating pancreatic cancer metastasis in preclinical mouse models. Its application is invaluable for research focused on pancreatic cancer and the underlying mechanisms of tumor progression.
  15. ALDH1A Inhibitor

    ALDH1A Inhibitor 673A is a selective inhibitor targeting ALDH1A1, ALDH1A2, and ALDH1A3, with IC50 values of 246 nM, 230 nM, and 348 nM, respectively. This compound demonstrates minimal inhibitory effects on other ALDH family members. It has been shown to induce necroptotic death in ovarian cancer stem-like cells and cause DNA double strand breaks in cancer cells. ALDH1A Inhibitor 673A serves as a valuable tool for researching ovarian cancer mechanisms and treatment strategies.
  16. Somatostatin Receptor Antagonist

    Cyclosomatostatin is a potent somatostatin receptor antagonist that specifically targets somatostatin receptor type 1 (SSTR1). This compound effectively inhibits SSTR1 signaling, leading to reduced cell proliferation, decreased ALDH+ cell population size, and diminished sphere formation in colorectal cancer cells. It serves as a valuable tool for research applications focused on understanding the role of somatostatin signaling in cancer biology.
  17. Oxidative/Nitrosative Stress Biomarker

    4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal recognized as a biomarker for oxidative and nitrosative stress. It acts as both a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2) and can modulate various signaling pathways by forming covalent adducts with nucleophilic sites on proteins, nucleic acids, and membrane lipids. This compound is implicated in cancer biology, particularly through its influence on mitochondrial function, making it a valuable tool for research in cellular stress responses and oncogenesis.
  18. ALDH Inhibitor

    4-Diethylaminobenzaldehyde is a reversible inhibitor of aldehyde dehydrogenases (ALDHs), exhibiting a Ki value of 4 nM specifically for ALDH1. This compound has demonstrated significant anti-androgenic activity with an IC50 of 1.71 μM. Its inhibitory effects on ALDH activities make it a valuable tool in biological research, particularly in studies focused on metabolic processes and hormonal regulation.
  19. ALDH1 Inhibitor

    ABD-3001 is a selective inhibitor of aldehyde dehydrogenase 1 (ALDH1). It has demonstrated potential in the study of refractory or relapsed acute myeloid leukemia and high-risk myelodysplastic syndrome. This compound may serve as a valuable tool for elucidating the role of ALDH1 in hematological malignancies and developing targeted therapies.
  20. Acohol use disorder

    Lefelsiran sodium is a small interfering RNA (siRNA) that targets aldehyde dehydrogenase 2 (ALDH2). It is utilized in research to investigate the mechanisms underlying alcohol use disorder. By downregulating ALDH2, Lefelsiran sodium may provide insights into metabolic pathways associated with alcohol consumption and the potential therapeutic approaches for treating alcohol-related conditions.
  21. ALDH1a2 Inhibitor

    Win 18446 is a selective inhibitor of the testes-specific enzyme ALDH1a2, exhibiting an IC50 of 0.3 μM. This compound effectively reverses spermatogenesis across various species and disrupts the biosynthesis of retinoic acid from retinol within the testes. It is valuable for research applications focused on reproductive biology and the modulation of retinoid signaling pathways.
  22. ALDH18A1 Inhibitor

    YG1702 is a selective inhibitor of ALDH18A1, a key enzyme involved in the biosynthesis of polyamines. This compound has demonstrated significant inhibitory effects on the proliferation of MYCN-amplified neuroblastoma cells and leads to down-regulation of MYCN expression. YG1702 binds to ALDH18A1 with high affinity, suggesting it may alter the enzyme’s activity and function. This reagent is valuable for research applications focused on neuroblastoma and cellular growth regulation.
  23. ALDH-2 Inhibitor

    CVT-10216 is a highly selective, reversible inhibitor of aldehyde dehydrogenase-2 (ALDH-2), demonstrating an IC50 of 29 nM. This compound also exhibits inhibitory effects on ALDH-1 with an IC50 of 1.3 μM. CVT-10216 has been shown to reduce excessive alcohol consumption in alcohol-preferring rat models and exhibits anxiolytic properties, making it valuable for research into alcohol use disorders and anxiety-related conditions.
  24. ALDH3A1 Inhibitor

    ALDH3A1-IN-3 is a selective inhibitor of the enzyme ALDH3A1, exhibiting a Ki value of 4.7 μM and an IC50 value of 16 μM. This compound shows no inhibitory activity against ALDH1A1, ALDH1A2, ALDH1A3, ALDH1B1, or ALDH2 in vitro. ALDH3A1-IN-3 is suitable for investigations in cellular oxidation processes and cancer research, making it a valuable tool for studying the role of ALDH3A1 in various biological contexts.
  25. ALDH3A1 Inhibitor

    ALDH3A1-IN-1 is a potent inhibitor of the aldehyde dehydrogenase 3A1 (ALDH3A1) enzyme, exhibiting an IC50 of 1.61 μM. This compound demonstrates superior efficacy compared to DEAB in targeting patient-derived primary prostate tumor epithelial cells, both as a standalone treatment and in combination with docetaxel. ALDH3A1-IN-1 is a valuable tool for investigating ALDH3A1's role in cancer biology and therapeutic resistance.
  26. ALDH1B1 Inhibitor

    IGUANA-1 is a selective inhibitor of ALDH1B1, exhibiting potent activity against this target. It demonstrates minimal mitochondrial toxicity, making it suitable for various experimental applications. Its antitumor properties position IGUANA-1 as a valuable compound for cancer research and drug development.
  27. ALDH1A3 Inhibitor

    ALDH1A3-IN-3 is a potent inhibitor of aldehyde dehydrogenase 1A3 (ALDH1A3), exhibiting an IC50 of 0.26 μM. This compound shows potential as a research tool for studying prostate cancer and can aid in understanding the role of ALDH1A3 in tumor biology. However, it functions as a substrate for ALDH3A1, which may limit its specificity as a selective inhibitor.
  28. ALDH1A3 Inhibitor

    ALDH1A3-IN-1 is a potent inhibitor of aldehyde dehydrogenase 1A3 (ALDH1A3), exhibiting an IC50 value of 0.63 μM and a Ki of 0.46 μM. This compound plays a significant role in cancer research, particularly in the study of prostate cancer, by modulating metabolic pathways associated with tumor progression. Researchers can utilize ALDH1A3-IN-1 to explore the implications of ALDH1A3 inhibition in cellular and molecular contexts pertaining to oncology.
  29. ALDH1A1 Inhibitor

    CM037 is a highly selective and competitive inhibitor of the enzyme ALDH1A1, with an IC50 of 4.6 μM. By blocking the catalytic activity of ALDH1A1, CM037 inhibits the activation of the HIF-1α/VEGF signaling pathway. This reagent is primarily utilized to investigate the role of ALDH1A1 in the regulation of cancer stem cells and angiogenesis, particularly in breast cancer models, highlighting its potential to obstruct tumor angiogenesis and stem cell properties.
  30. ALDH3A1 Inhibitor

    EN40 is a selective inhibitor of aldehyde dehydrogenase 3A1 (ALDH3A1), functioning as a covalent ligand with an IC50 value of 2 µM. This compound demonstrates significant inhibitory activity, making it a valuable tool for research focused on cellular metabolism and oxidative stress. Its application extends to the study of various diseases where ALDH3A1 plays a role, providing insights into potential therapeutic interventions.
  31. ALDH1A Inhibitor

    CM010 is a selective inhibitor of the aldehyde dehydrogenase 1A (ALDH1A) family, exhibiting IC50 values of 1700 nM, 740 nM, and 640 nM for ALDH1A1, ALDH1A2, and ALDH1A3, respectively. This compound does not inhibit other members of the ALDH family, making it a valuable tool for specific enzyme studies. CM010 demonstrates potential in regulating metabolic processes and exhibits anti-cancer activity, making it relevant for cancer research applications.
  32. Dehydrogenase

    ALDH (Aldehyde dehydrogenase (NAD(P))) is an enzyme that catalyzes the oxidation of aldehydes into their corresponding carboxylic acids, simultaneously reducing the cofactors NAD(P) to NAD(P)H. This enzymatic activity is crucial for cellular detoxification and metabolism, making ALDH significant in biochemical research. It is frequently employed in studies investigating aldehyde stress responses and metabolic pathways related to aldehyde processing.
  33. ALDH1A3 Inhibitor

    ALDH1A3-IN-2 is a selective inhibitor of aldehyde dehydrogenase 1A3 (ALDH1A3) with an IC50 of 1.29 μM. This compound demonstrates significant potential for studying the role of ALDH1A3 in various malignancies, particularly in prostate cancer where ALDHs are frequently overexpressed. ALDH1A3-IN-2 can be utilized in research focusing on cancer pathways and therapeutic strategies targeting ALDH-related enzymatic activity.
  34. ALDH1A3 Inhibitor

    MCI-INI-3 is a selective competitive inhibitor of human ALDH1A3, exhibiting a Ki value of 0.55 μM for ALDH1A3 and a Ki value of 78.2 μM for ALDH1A1. This compound effectively disrupts retinoic acid biosynthesis, leading to a reduction in viability of glioblastoma stem cells GSC-83 and GSC-326. MCI-INI-3 is a valuable tool for research focused on cancer biology and the therapeutic targeting of glioblastoma.
  35. ALDH1A3 Inhibitor

    KOTX1 is a selective inhibitor of the ALDH1A3 enzyme, demonstrating oral bioactivity. This compound has been shown to enhance glucose tolerance, promote insulin secretion, and regulate blood sugar levels in diabetic mouse models. KOTX1 is a valuable tool for investigating metabolic disorders and the role of ALDH1A3 in diabetes research.
  36. aldh1a1 Inhibitor

    ALDH1A1-IN-2 is a selective inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), an enzyme crucial for the oxidation of cytotoxic aldehydes. By inhibiting ALDH1A1, this compound may contribute to studies focusing on cancer, inflammation, and obesity-related pathways. Its biological activity positions it as a valuable tool for researchers investigating the roles of ALDH enzymes in diverse pathophysiological conditions.
  37. aldehyde dehydrogenase inhibitor

    Nitrefazole is a 4-nitroimidazole derivative functioning as a potent inhibitor of aldehyde dehydrogenase (ALDH). It exhibits strong and sustained inhibition of ALDH, an enzyme critical in alcohol metabolism. This compound is valuable for research applications focused on alcoholism, metabolic studies, and pharmacological modulation of ALDH activity.
  38. Stable Isotope

    4-Hydroxynonenal-d3 is a deuterated form of 4-Hydroxynonenal, an α,β-unsaturated hydroxyalkenal recognized as a biomarker for oxidative and nitrosative stress. It serves as both a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2), influencing various signaling pathways by forming covalent adducts with nucleophilic sites in proteins, nucleic acids, and membrane lipids. As a significant player in cancer biology, 4-Hydroxynonenal impacts mitochondrial function and cellular signaling processes, making it valuable for research in oxidative stress and its implications in disease.
  39. Aldehyde Dehydrogenase (ALDH) Inhibitor

    S-Methyl-N,N-diethylthiolcarbamate is an effective inhibitor of aldehyde dehydrogenase (ALDH). This compound serves as the active metabolite of the aldehyde dehydrogenase inhibitor disulfiram, generated through the methylation of diethyldithiocarbamate in mouse liver microsomes. S-Methyl-N,N-diethylthiolcarbamate exhibits significant biological activity, demonstrated by its ability to inhibit rat liver low Km ALDH with an ID50 value of 15.5 mg/kg. In vivo studies indicate that a dose of 20.6 mg/kg can reduce mean arterial pressure and elevate heart rate in rats under ethanol stimulation, highlighting its potential applications in cardiovascular and metabolic research.
  40. ALDH1A2 Inhibitor

    ALDH1A2-IN-1 is a reversible inhibitor targeting the active site of ALDH1A2, demonstrating an IC50 of 0.91 μM and a Kd of 0.26 μM. This compound is characterized by multiple hydrophobic interactions, making it an effective tool for studying the enzyme's role in biological pathways. It is applicable in research focused on cancer metabolism, stem cell differentiation, and neurotransmitter synthesis modulation.
  41. ALDH1 B1 Inhibitor

    IGUANA-1 free base is a selective inhibitor of aldehyde dehydrogenase 1 B1 (ALDH1 B1) with an IC50 value of 30 nM. This compound demonstrates significant anti-proliferative activity against SW480 colorectal cancer cells, achieving IC50 values of 2.46 μM under adherent conditions and 0.39 μM in spheroid cultures. IGUANA-1 free base is a valuable tool for cancer research, particularly in studying the role of ALDH1 B1 in tumor growth and progression.
  42. ALDH-2/MAO Inhibitor

    7-Hydroxy-4-phenylcoumarin is a dual inhibitor of aldehyde dehydrogenase-2 (ALDH-2) and monoamine oxidase (MAO), demonstrating IC50 values of 1.5 µM and 0.5 µM, respectively. This compound exhibits significant biological activity that may influence cellular metabolism and neurotransmitter regulation. It is suitable for research applications focused on neuroprotection and metabolic studies.
  43. ALDH2 Agonist

    ALDH2 activator 1 is an allosteric agonist of aldehyde dehydrogenase 2 (ALDH2). This compound enhances cardiac function and mitigates myocardial necrosis in murine models of myocardial ischemia-reperfusion. It holds potential for advancing research in cardiovascular diseases, particularly in the context of myocardial infarction.
  44. ALDH Enhancer

    Taraxerone is an ALDH enhancer derived from Sedum sarmentosum. It significantly increases the activities of alcohol dehydrogenase (ADH) and acetaldehyde dehydrogenase (ALDH), exhibiting EC50 values of 512.42 μM and 500.16 μM, respectively. This compound is valuable for studies focused on alcohol metabolism and enzyme regulation in biochemical research.
  45. ALDH1A1 Inhibitor

    FSI-TN42 is a selective, irreversible inhibitor of ALDH1A1 with an IC50 of 23 nM, demonstrating significant potency with an 800-fold preference over ALDH1A2. This compound is valuable for research applications targeting metabolic pathways involving aldehyde dehydrogenases, particularly in cancer and stem cell studies. Its oral bioavailability makes it a suitable candidate for in vivo investigations of ALDH1A1's role in various biological processes.
  46. Acetaldehyde Dehydrogenase Inhibitor

    Coprine is a mycotoxin derived from Coprinopsis atramentaria that functions as an inhibitor of acetaldehyde dehydrogenase. By inhibiting this enzyme, coprine leads to the accumulation of acetaldehyde, which can trigger the alcohol flushing reaction in susceptible individuals. This compound is useful in research focused on alcohol metabolism and the effects of acetaldehyde accumulation on physiological processes.
  47. Aldehyde Dehydrogenase 2 Activator

    Mirivadelgat is an activator of aldehyde dehydrogenase 2 (ALDH2), which plays a crucial role in detoxifying aldehydes and maintaining cellular homeostasis. This compound exhibits potential biological activity in the investigation of interstitial lung disease, pulmonary hypertension, and various cancer models. Mirivadelgat serves as a valuable tool for researchers studying metabolic pathways and therapeutic approaches related to these conditions.
  48. ALDH1A1 Inhibitor

    ALDH1A1-IN-4 is a potent inhibitor of aldehyde dehydrogenase (ALDH) A1, demonstrating an IC50 value of 0.32 μM. This compound is significant in cancer research, offering insights into pathways involving ALDH1A1's role in tumor biology and potential therapeutic strategies. Its inhibitory activity may contribute to the understanding of cancer metabolism and the development of novel treatments.
  49. ALDH1A2 Inhibitor

    CM121 is a reversible inhibitor of ALDH1A2, featuring a competitive mechanism with an IC50 of 0.54 μM and a Kd of 1.1 μM. This compound demonstrates significant hydrophobic interactions at the active site, making it a valuable tool for studying ALDH1A2's role in various biological processes. It is suitable for applications in cancer research and stem cell biology, where modulation of aldehyde dehydrogenase activity is of interest.
  50. Acohol use disorder

    Lefelsiran is a small interfering RNA (siRNA) that specifically targets aldehyde dehydrogenase 2 (ALDH2). This reagent is primarily employed in research focused on alcohol use disorder, investigating the molecular mechanisms underlying this condition. By modulating ALDH2 expression, Lefelsiran facilitates the study of its role in alcohol metabolism and the potential therapeutic interventions for alcohol dependence.

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