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Aldh Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Aldehyde Dehydrogenase (ALDH) (34) Apoptosis (4) Bacterial (1) Chemerin Receptor (1) Cholinesterase (ChE) (1) Cuproptosis (1) Endogenous Metabolite (2) Fungal (1) Interleukin Related (1) Isotope-Labeled Compounds (1) Mitochondrial Metabolism (1) Necroptosis (1) Pyroptosis (1) Reverse Transcriptase (1) Somatostatin Receptor (2)
By Research Areas:	Cancer (29) Cardiovascular Disease (2) Endocrinology (2) Infection (1) Inflammation/Immunology (1) Metabolic Disease (4) Neurological Disease (2)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Aldehyde Dehydrogenase (ALDH)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-157567

FSI-TN42

N42
Aldehyde Dehydrogenase (ALDH) Metabolic Disease

ALDH1A1/2-IN-1 is an ALDH1A1 and ALDH1A2 inhibitor that can be used for preventing spermatogenesis .

FSI-TN42 N42	Aldehyde Dehydrogenase (ALDH)	Metabolic Disease
ALDH1A1/2-IN-1 is an *ALDH1A1* and *ALDH1A2* inhibitor that can be used for preventing spermatogenesis .

HY-W017186

ALDH1A3-IN-3	Aldehyde Dehydrogenase (ALDH)	Cancer
ALDH1A3-IN-3 (compound 16) is a potent inhibitor of *ALDH1A3, with an IC₅₀* of 0.26 μM. ALDH1A3-IN-3 is also a good ALDH3A1 substrate. ALDH1A3-IN-3 can be used for the research of prostate cancer .

HY-122912

ALDH1A inhibitor 673A Aldh1Ai 673A	Aldehyde Dehydrogenase (ALDH) Necroptosis	Cancer
ALDH1A inhibitor 673A is an *ALDH1A* inhibitor. ALDH1A inhibitor 673A inhibits all three ALDH1A family members (IC₅₀: 246 nM, 230 nM, 348 nM for ALDH1A1, ALDH1A2, ALDH1A3 respectively. ALDH1A inhibitor 673A induces necroptotic cell death preferentially in CD133+ ovarian CSCs. ALDH1A inhibitor 673A also inhibits chemotherapy-resistant tumor growth .

HY-158026

ALDH1A1-IN-5	Aldehyde Dehydrogenase (ALDH)	Cancer
ALDH1A1-IN-5 (compound 25) is a potent aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitor with EC₅₀ value of 83, 45, 43 µM for ALDH1A1, ALDH1A2, ALDH1A3, respectively. ALDH1A1-IN-5 has the potential for the research of high-grade serous ovarian cancer (HGSOC) .

HY-144671

ALDH3A1-IN-2	Aldehyde Dehydrogenase (ALDH)	Cancer
ALDH3A1-IN-2 (Compound 19) is a potent inhibitor of *ALDH3A1* with an IC₅₀ of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH3A1-IN-2 has the potential for the research of cancer diseases .

HY-144669

ALDH1A3-IN-2	Aldehyde Dehydrogenase (ALDH)	Cancer
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 .

HY-144667

ALDH1A3-IN-1	Aldehyde Dehydrogenase (ALDH)	Cancer
ALDH1A3-IN-1 (Compound 14) is a potent *ALDH1A3* inhibitor, with an IC₅₀ of 0.63 µM and a K_i of 0.46 µM. ALDH1A3-IN-1 can be studied in prostate cancer .

HY-157872

ALDH1A1-IN-4	Aldehyde Dehydrogenase (ALDH)	Cancer
ALDH1A1-IN-4 (compound A1) is a potent inhibitor of aldehyde dehydrogenase (ALDH) A1, with IC₅₀ value of 0.32 μM. ALDH1A1-IN-4 plays an important role in cancer research .

HY-146240

ALDH1A1-IN-3	Aldehyde Dehydrogenase (ALDH)	Metabolic Disease
ALDH1A1-IN-3 (compound 57) is an excellent and selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitor with an IC₅₀ value of 0.379 μM. ALDH1A1-IN-3 can effectively improve glucose consumption in HepG2 cells. ALDH1A1-IN-3 can be used for researching glucose metabolism improvement .

HY-135841

CM10	Aldehyde Dehydrogenase (ALDH)	Metabolic Disease Cancer
CM10 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. CM10 does not inhibit any of the other ALDH family members. CM10 can regulate metabolism and has anti-cancer activity .

HY-144670

ALDH3A1-IN-1	Aldehyde Dehydrogenase (ALDH)	Cancer
ALDH3A1-IN-1 (Compound 18) is a potent inhibitor of *ALDH3A1* with an IC₅₀ of 1.61 μM. ALDH3A1-IN-1 is more potent than DEAB against patient-derived primary prostate tumor epithelial cells, as single agents or in combination research with docetaxel .

HY-126003

ALDH1A1-IN-2	Aldehyde Dehydrogenase (ALDH)	Cancer
ALDH1A1-IN-2 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 (extracted from patent WO2019089626A1, compound 295) .

HY-139031

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

HY-19801

CVT-10216 1 Publications Verification
CVT-10216 is a highly selective, reversible aldehyde dehydrogenase-2 (ALDH-2) inhibitor with an IC₅₀ of 29 nM. CVT-10216 also has inhibitory effect of ALDH-1 with an IC₅₀ of 1.3 μM. CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects .

HY-N0018

Daidzin 5 Publications Verification Daidzoside; NPI-031D; Daidzein 7-O-glucoside	Mitochondrial Metabolism Reverse Transcriptase Aldehyde Dehydrogenase (ALDH)	Others
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 .

HY-156443

YG1702	Aldehyde Dehydrogenase (ALDH)	Cancer
YG1702 is a potent *ALDH18A1*-specific inhibitor. YG1702 attenuates the growth of MYCN-amplified NB and down-regulates MYCN. YG1702 physically interacts with ALDH18A1 with a high affinity and might potentially affect its enzymatic activity .

HY-146683

KS106	Aldehyde Dehydrogenase (ALDH) Apoptosis	Cancer
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 .

HY-146682

KS100	Aldehyde Dehydrogenase (ALDH) Apoptosis	Cancer
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 .

HY-B0364A

Dyclonine hydrochloride 1 Publications Verification Dyclocaine hydrochloride	Bacterial Fungal Aldehyde Dehydrogenase (ALDH)	Infection Cancer
Dyclonine (Dyclocaine) hydrochloride is an orally effective *ALDH* covalent inhibitor (crosses blood-brain barrier), with an IC₅₀ of 35 µM for *ALDH2* and 76 µM for *ALDH3A1. Dyclonine hydrochloride has sensitizing activities for targeted cancer cells and antibacterial. Dyclonine hydrochloride is also a local anesthetic that blocks the transmission of various nerve impulses or stimuli and inhibits* the sensation of touch and pain .

HY-W016645

4-Diethylaminobenzaldehyde 1 Publications Verification	Aldehyde Dehydrogenase (ALDH)	Cancer
4-Diethylaminobenzaldehyde is a reversible aldehyde dehydrogenases (ALDHs) inhibitor, with a K_i of 4 nM for ALDH1. 4-Diethylaminobenzaldehyde displays potent anti-androgenic effect (IC₅₀= 1.71μM) .

HY-18768

NCT-501 4 Publications Verification	Aldehyde Dehydrogenase (ALDH)	Cancer
NCT-501 is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC₅₀ of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC₅₀ >57 μM).

HY-18768A

NCT-501 hydrochloride	Aldehyde Dehydrogenase (ALDH)	Cancer
NCT-501 hydrochloride is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC₅₀ of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC₅₀ >57 μM) .

HY-112278

NCT-506

Aldehyde Dehydrogenase (ALDH) Cancer

NCT-506 is an orally bioavailable aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with an IC₅₀ of 7 nM .
HY-110294

CM037

A37
Aldehyde Dehydrogenase (ALDH) Cancer

CM037 is a selective inhibitor of ALDH1A1 (aldehyde dehydrogenase 1A1) with an IC₅₀ of 4.6 µM .
HY-122577

EN40

Aldehyde Dehydrogenase (ALDH) Cancer

EN40 is a potent, selective aldehyde dehydrogenase 3A1 (ALDH3A1) inhibitor as a covalent ligand, exhibits an IC₅₀ value of 2 uM
HY-139032

CM121

Aldehyde Dehydrogenase (ALDH) Others

CM121 is an active site-directed reversible ALDH1A2 inhibitor (IC₅₀=0.54 μM；Kd=1.1 μM) with a variety of hydrophobic interactions .

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

CM037 A37	Aldehyde Dehydrogenase (ALDH)	Cancer
CM037 is a selective inhibitor of *ALDH1A1* (aldehyde dehydrogenase 1A1) with an IC₅₀ of 4.6 µM .

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

CM121	Aldehyde Dehydrogenase (ALDH)	Others
CM121 is an active site-directed reversible *ALDH1A2* inhibitor (IC₅₀=0.54 μM；Kd=1.1 μM) with a variety of hydrophobic interactions .

HY-148466

IGUANA-1	Aldehyde Dehydrogenase (ALDH)	Cancer
IGUANA-1 is a potent inhibitor of *ALDH1B1*, which is a mitochondrial enzyme that promotes colorectal and pancreatic cancer. IGUANA-1 has significant inhibition against cancer cells .

HY-P1201

Cyclosomatostatin	Somatostatin Receptor	Cancer
Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells .

HY-W011094

Win 18446 1 Publications Verification	Aldehyde Dehydrogenase (ALDH)	Endocrinology
Win 18446 is an orally active testes-specific enzyme ALDH1a2 inhibitor, with an IC₅₀ of 0.3 μM. Win 18446 reversibly inhibits spermatogenesis in many species and inhibits Retinoic acid (HY-14649) biosynthesis from Retinol (HY-B1342) within the testes .

HY-112277

NCT-505	Aldehyde Dehydrogenase (ALDH)	Cancer
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).

HY-126241

RV01	Aldehyde Dehydrogenase (ALDH)	Inflammation/Immunology
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 .

HY-P1201A

Cyclosomatostatin TFA	Somatostatin Receptor	Cancer
Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells .

HY-148243

IGUANA-1 free base STL5-T-0057	Aldehyde Dehydrogenase (ALDH)	Cancer
IGUANA-1 free base (STL5-T-0057) is an selective ALDH1 B1 inhibitor with an IC₅₀ value of 30 nM. IGUANA-1 free base inhibits cell growth of SW480 cells in adherent and spheroid conditions with IC₅₀ values of 2.46 and 0.39 μM, respectively. IGUANA-1 free base can be used for the research of cancer .

HY-B0240

Disulfiram Maximum Cited Publications 49 Publications Verification Tetraethylthiuram disulfide; TETD	Aldehyde Dehydrogenase (ALDH) Interleukin Related Pyroptosis Apoptosis Cuproptosis	Metabolic Disease Cancer
Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells. Disulfiram, a copper ion carrier, with Cu ²⁺ increases intracellular ROS levels and induces cuproptosis .

HY-138097

α-NETA 5+ Cited Publications	Chemerin Receptor Aldehyde Dehydrogenase (ALDH) Cholinesterase (ChE) Apoptosis	Cancer
α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC₅₀ of 9 μM. α-NETA is a potent ALDH1A1 (IC₅₀=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC₅₀=84 µM) and acetylcholinesterase (AChE; IC₅₀=300 µM). α-NETA has anti-cancer activity .

HY-113466

4-Hydroxynonenal 5 Publications Verification 4-HNE	Aldehyde Dehydrogenase (ALDH) Endogenous Metabolite	Cardiovascular Disease Neurological Disease Cancer
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 .

HY-113466S

4-Hydroxynonenal-d3 4-HNE-d₃	Isotope-Labeled Compounds Aldehyde Dehydrogenase (ALDH) Endogenous Metabolite	Cardiovascular Disease Neurological Disease Cancer
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[1][2][3].

Cyclosomatostatin	Somatostatin Receptor	Cancer
Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells .

Cyclosomatostatin TFA	Somatostatin Receptor	Cancer
Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0018

Daidzin 5 Publications Verification Daidzoside; NPI-031D; Daidzein 7-O-glucoside	Structural Classification Monophenols Flavonoids Classification of Application Fields Leguminosae Glycine max (L.) merr Source classification Other Diseases Phenols Plants Disease Research Fields Isoflavones	Mitochondrial Metabolism Reverse Transcriptase Aldehyde Dehydrogenase (ALDH)
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 .

HY-113466

4-Hydroxynonenal 5 Publications Verification 4-HNE	Structural Classification Neurological Disease Classification of Application Fields Ketones, Aldehydes, Acids Disease markers Nervous System Disorder Endogenous metabolite Disease Research Fields Cancer	Aldehyde Dehydrogenase (ALDH) Endogenous Metabolite
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 .

Cat. No.	Product Name	Chemical Structure

HY-113466S

4-Hydroxynonenal-d3
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[1][2][3].

4-Hydroxynonenal-d3

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[1][2][3].

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