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Drug Metabolite Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S2205 DesMethyl Erlotinib (OSI-420) HCl DesMethyl Erlotinib (OSI-420) HCl is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM).
Drug Metab Dispos, 2025, 53(5):100069
J Pharm Biomed Anal, 2023, 236:115716
Front Oncol, 2022, 12:939118
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S1501 Mycophenolate mofetil Mycophenolate mofetil is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively. This compound induces caspase-dependent apoptosis and cell cycle inhibition in multiple myeloma cells.
Cell Metab, 2025, S1550-4131(25)00482-6
Cancers, 2025, 3389
Haematologica, 2024, 109(12):3989-4006
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S4785 Nicotinamide N-oxide Nicotinamide N-oxide (Nicotinamide 1-oxide, 1-oxynicotinamide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. This compound is novel, potent, and selective antagonists of the CXCR2 receptor.
Front Immunol, 2025, 16:1552993
Inflammation, 2024,
Cell Rep, 2023, 42(6):112566
S6889 Monomethyl Fumarate Monomethyl Fumarate (MMF, Monomethylfumarate, Fumaric acid monomethyl ester, Methyl hydrogen fumarate), the active metabolite of the psoriasis drug Fumaderm, is a potent GPR109A agonist. This compound prevents major dysfunctions associated with neurodegenerative diseases: oxidative stress, mitochondrial dysfunction, apoptosis and autophagy.
Frontiers in Oncology, January 28, 2020, 22
Cell Cycle, December 8, 2022, 818-828
Cell Cycle, 2023, 818-828
S3698 Nortriptyline hydrochloride Nortriptyline hydrochloride (Desitriptyline, ELF-101, EN-7048, Desmethylamitriptyline) is the hydrochloride salt form of nortriptyline, a tricyclic antidepressant agent used for short-term treatment of various forms of depression.
Frontiers in Bioinformatics, September 14, 2021, 710591
EMBO Molecular Medicine, December 23, 2025, 433-461
EMBO Molecular Medicine, December 23, 2025, Epub ahead of print
S5840 Palifosfamide Palifosfamide (ZIO-201, Isophosphamide mustard) is a novel DNA alkylator and the active metabolite of ifosfamide with potential antineoplastic activity.
Oncotarget, April 27, 2018, 22571-22585
bioRxiv, April 21, 2025, nan
S4207 Clofibric Acid Clofibric acid(Chlorofibrinic acid) is a PPARα agonist and hypolipidemic agent.
Laboratory Investigation, 2023, 100004
Lab Invest, 2023, 103(1):100004
S6601 (±)-Equol (±)-Equol, an isoflavandiol estrogen, is a metabolite of the soy isoflavones, daidzin and daidzein.
E4607 Oseltamivir acid Oseltamivir acid(GS 4071,Ro 64-0802,Oseltamivir carboxylate), a metabolite of the antiviral compound oseltamivir, acts as a competitive inhibitor of influenza neuraminidases A and influenza neuraminidases B with IC50 of 0.1 to 4.9 nM respectively, thereby preventing virus budding and release.
S0320 Cycloguanil hydrochloride Cycloguanil hydrochloride, an active metabolite of proguanil, acts on malaria schizonts in erythrocytes and hepatocytes.
E0680 Deslanoside Deslanoside(Desacetyllanatoside C) is a cardenolide glycoside, has the effects of anti-arrhythmia and cardiotonic, also is used as an EC 3.6.3.9 (Na+/K+-transporting ATPase) inhibitor. 
S5834 p-Coumaric acid ethyl ester p-Coumaric acid ethyl ester is the ethyl ester of p-Coumaric acid, which is a plant metabolite which exhibits antioxidant and anti-inflammatory properties.
S6438 Ufiprazole Ufiprazole (Omeprazole sulfide) is an intermediate used in the production of the gastric proton pump inhibitors omeprazole and esomeprazole.
S4509 4-Aminoantipyrine 4-Aminoantipyrine(Ampyrone) is a metabolite of aminopyrine with analgesic, anti-inflammatory, and antipyretic properties. It is used as a reagent for biochemical reactions producing peroxides or phenols.
S0225 IMR-1A IMR-1A, an acid metabolite of IMR-1, is a potent inhibitor of Notch with IC50 of 0.5 μM and Kd of 2.9 μM. This compound exhibits anti-tumor activity.
S5437 4,4'-DDE 4,4'-DDE (DDE, p,p'-DDE, p,p'-dichlorodiphenyldichloroethylene), a breakdown product of DDT, is an organochlorine pesticide and may behave as a potent androgen receptor antagonist.