Inhibitors

Selective Enzyme & Receptor Inhibitors for Drug Discovery

A comprehensive portfolio of high-purity enzyme inhibitors including kinase inhibitors, protease inhibitors, epigenetic inhibitors, phosphodiesterase inhibitors, GPCR antagonists, ion channel blockers, and metabolic enzyme inhibitors for target validation, pathway dissection, and drug discovery. These rigorously validated enzyme inhibitors come with full IC50 and selectivity data, complete analytical documentation, and reliable global delivery.

🎯 Target Validation 📊 IC50 & Selectivity Data 🔨 Custom Synthesis ⚡ Fast Global Shipping

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What Are Inhibitors?

An inhibitor is a compound that binds to an enzyme or receptor and reduces or blocks its biological activity. Enzyme inhibitors are the most widely used class of pharmacological tools, serving as positive controls in screening assays, reference compounds for potency comparisons, tool compounds for target validation and pathway dissection, and lead molecules for drug development. These enzyme inhibitors are classified by mechanism: competitive (bind active site), non-competitive (bind allosteric site), uncompetitive (bind enzyme-substrate complex), and irreversible (form covalent bond).

At ACUBIOCHEM, we offer one of the most comprehensive inhibitor portfolios in the industry, covering kinase inhibitors (receptor tyrosine kinases, serine/threonine kinases, lipid kinases — EGFR, VEGFR, PI3K, AKT, mTOR, CDK, JAK, BTK, and 200+ more), protease inhibitors (serine, cysteine, aspartyl, metalloproteases — DPP-4, ACE, MMP, caspase, cathepsin, proteasome), epigenetic inhibitors (HDAC, BET, EZH2, DNMT, LSD1), phosphodiesterase inhibitors, GPCR antagonists, ion channel blockers, and metabolic enzyme inhibitors. Each compound is manufactured to ≥95% purity and accompanied by validated IC50, Ki, and selectivity data.

"The right inhibitor at the right concentration is the key to clean, reproducible target validation. Our portfolio covers all major target classes with documented potency and selectivity profiles, so you can choose with confidence and avoid off-target artifacts."

Whether you need a well-characterized tool compound for a classic target, a selective inhibitor for an emerging target, or a custom analog for SAR studies, our comprehensive catalog and custom synthesis capabilities support your research from initial target identification through preclinical development.

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Inhibitor

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Target

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Blockade

Selective tools for target validation and pathway dissection

Target Classes & Inhibition Mechanisms

Our inhibitor portfolio spans all major target classes in drug discovery. Explore the mechanisms, key target families, and therapeutic applications below.

🎯 Kinase Inhibitors

ATP-competitive, allosteric, or irreversible inhibitors of protein and lipid kinases — the most extensively targeted enzyme family in modern drug discovery. Covers receptor tyrosine kinases, serine/threonine kinases, and lipid kinases critical for cell signaling and proliferation.

Receptor TKs Ser/Thr Kinases Lipid Kinases Oncology Inflammation

🧬 Protease Inhibitors

Active-site or allosteric inhibitors of proteolytic enzymes classified by catalytic mechanism: serine, cysteine, aspartyl, and metalloproteases. Essential tools for studying protein processing, degradation, viral replication, and inflammatory signaling cascades.

Serine Proteases Cysteine Proteases Metalloproteases Virology Inflammation

🧋 Epigenetic Inhibitors

Inhibitors of epigenetic regulators including histone deacetylases (HDAC), bromodomain and extra-terminal (BET) proteins, histone methyltransferases, and DNA methyltransferases (DNMT). Powerful tools for studying chromatin modification and gene expression regulation.

HDAC BET Bromodomain EZH2 / DNMT Oncology Immunology

⚙ Other Key Target Classes

Additional major inhibitor classes covering phosphodiesterases, metabolic enzymes, GPCR antagonists, ion channel blockers, and heat shock protein inhibitors. Diverse target families spanning multiple therapeutic areas and biological pathways.

Phosphodiesterases Metabolic Enzymes GPCR Antagonists Ion Channels Cross-therapeutic

Common Research Applications

Our enzyme inhibitors power critical workflows across drug discovery, cell biology, and translational research, with validated potency and selectivity for reliable target validation.

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Target Validation

Selective inhibitors to confirm target involvement in disease pathways, phenotypic responses, and therapeutic hypothesis testing with appropriate controls

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Signaling Pathway Dissection

Tool compounds to map signaling cascades, identify downstream effectors, establish causal relationships, and differentiate pathway-specific vs. off-target effects

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Screening & Assay Development

Positive and reference controls in HTS, enzyme kinetics, cell-based assays, high-content phenotypic screening, and counter-screen panels for selectivity profiling

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Drug Discovery & Development

Lead compounds for SAR optimization, combination therapy studies, PK/PD modeling, preclinical efficacy and toxicity evaluation, and clinical candidate selection

Why Researchers Choose ACUBIOCHEM

Rigorously validated inhibitors you can trust for reproducible target validation and drug discovery.

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Assured Quality

≥95% purity verified by HPLC and NMR, with chiral HPLC verification for stereochemically critical compounds and COA for every batch

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Validated Potency

IC50, Ki, and selectivity data from peer-reviewed literature or validated in-house assays, including kinase selectivity panel data where available

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Full Documentation

Structure, physicochemical properties, solubility, DMSO stability, storage conditions, and safety information included with every order and on product pages

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Global Supply & Libraries

Inventory maintained for rapid worldwide delivery, with bulk and custom packaging, and pre-assembled screening libraries (kinase, epigenetic, FDA-approved)

Frequently Asked Questions

Answers to common questions about our inhibitors, potency data, and technical support.

What purity standards do your inhibitors meet? +

Our inhibitors typically meet ≥95% purity as verified by HPLC and NMR analysis. Each compound ships with a Certificate of Analysis (COA) detailing exact purity, lot number, and analytical results. For kinase inhibitors and other compound classes where stereochemistry is critical for target binding, we also verify enantiomeric purity by chiral HPLC. For compounds with known polymorphs or salt forms, we verify identity by XRPD or ion chromatography. For custom synthesis projects or research-grade requirements, ≥98% purity and additional characterization (HRMS, elemental analysis) are available upon request.

Do you provide IC50, Ki, and selectivity data? +

Yes. Where available, we include IC50, Ki, and selectivity data sourced from peer-reviewed literature or validated in-house assays. We note assay conditions (enzyme construct, substrate concentration, readout method, cell line) so you can compare data across compounds and assess relevance to your experimental system. We are continuously expanding our in-house profiling data, including kinase selectivity panels (400+ kinases at 1 μM), off-target screening against common anti-targets (hERG, CYP, kinases), and cell-based potency data (pIC50, pEC50). Contact our technical team for specific compound data sheets or to request custom profiling.

What target classes are covered in your inhibitor portfolio? +

Our inhibitor catalog covers all major target classes in drug discovery: protein kinases (EGFR, VEGFR, PDGFR, FGFR, MET, ALK, ROS1, RET, PI3K, AKT, mTOR, CDK, JAK, BTK, SYK, FLT3, Aurora, PLK, MEK, ERK, GSK3, PKC, PKA, AMPK, and 200+ more), proteases (DPP-4, ACE, MMP, ADAM, caspase, cathepsin, calpain, proteasome, renin, thrombin, factor Xa), epigenetic targets (HDAC I/II/IV, SIRT, BET, CBP/p300, EZH2, EHMT1/2, DOT1L, LSD1, DNMT, PRMT), phosphodiesterases (PDE1-10), metabolic enzymes (HMGCR, DPP-4, aldose reductase, 11β-HSD, PTP1B), GPCRs (adrenergic, dopaminergic, histaminergic, serotonergic, opioid, cannabinoid, purinergic), ion channels (calcium, potassium, sodium, chloride), and heat shock proteins (HSP90, HSP70). New inhibitors are added weekly.

Can you synthesize custom inhibitor analogs or focused libraries? +

Absolutely. Our medicinal chemistry team specializes in custom inhibitor synthesis, including structural analogs for SAR studies (hit-to-lead and lead optimization), functional selectivity or biased ligands, allosteric modulators, covalent inhibitors with custom warheads, bifunctional degraders (PROTACs, molecular glues), isotopically labeled compounds (for MS-based target engagement and ADME studies), photoaffinity probes (for target identification), and focused screening libraries around a specific scaffold or target class. We also offer pre-assembled libraries: kinase inhibitor library (300+ compounds), epigenetic compound library, FDA-approved drug library (2000+), natural product library, and custom-designed panels. Share your target structure, scaffold, or library requirements, and we'll provide a feasibility assessment and quote within 48 hours.

How should inhibitors be stored and handled for optimal potency? +

Most inhibitors are shipped at ambient temperature and should be stored at −20°C in the dark upon receipt. Some light-sensitive, oxidation-prone, or hygroscopic compounds require −80°C storage under inert atmosphere (argon or nitrogen). We recommend reconstituting in DMSO (most inhibitors are DMSO-soluble) or the appropriate aqueous buffer immediately before use and aliquoting to avoid repeated freeze-thaw cycles, which can degrade compound potency and promote precipitation. For long-term storage of DMSO stocks, we recommend −80°C and protection from light. Detailed storage, solubility (in DMSO, water, and common buffers), DMSO stability (at −20°C, 4°C, and room temperature), and handling information is provided on each product page and with every order. Our technical team can help you optimize compound handling, solubility enhancement, and assay conditions for your specific target and experimental system.

Do you offer selectivity profiling and off-target screening services? +

Yes. We offer comprehensive selectivity profiling services to help you characterize your inhibitor's specificity and identify potential off-target activities. Our services include: kinase selectivity panels (400+ human kinases tested at 1 μM or 10 μM, with IC50 determination for hits), broader off-target panels (GPCRs, ion channels, transporters, nuclear receptors), CYP inhibition profiling (CYP1A2, 2C9, 2C19, 2D6, 3A4), hERG binding and functional assays, and custom target panels designed around your therapeutic area. We also offer cell-based selectivity profiling (panel of cancer cell lines, primary cell toxicity, cytokine profiling). All profiling is performed in GLP-compliant or research-grade facilities with full data reporting and analysis. Contact our technical team for panel design, pricing, and turnaround time.

What is the difference between reversible and irreversible inhibitors? +

Reversible inhibitors bind non-covalently to their target and can be displaced by substrate or competing compounds. They are further classified as competitive (bind the active site, compete with substrate, Km increases, Vmax unchanged), non-competitive (bind an allosteric site, reduce enzyme activity, Vmax decreases, Km unchanged), uncompetitive (bind only the enzyme-substrate complex, both Km and Vmax decrease), and mixed (bind both free enzyme and ES complex with different affinities). Irreversible inhibitors form covalent bonds with target residues (often cysteine, serine, or lysine), permanently inactivating the enzyme. They include mechanism-based (suicide) inhibitors that are activated by the enzyme's catalytic machinery, and affinity labels that react with nucleophilic residues near the binding site. Irreversible inhibitors often show prolonged pharmacodynamic effects (target recovery requires new protein synthesis) but may have higher off-target reactivity risk. The choice depends on your target, therapeutic goal, and safety considerations. Our technical team can help you select the appropriate inhibitor type and design covalent analogs with specific warheads.

Need a Custom Inhibitor or Screening Library?

Our medicinal chemists and technical support team are ready to help you select the right inhibitor, synthesize a custom analog or PROTAC, or assemble a focused screening library for your drug discovery program.

Request Custom Synthesis Contact Technical Support