Enzyme Inhibitors
Tim HiddemannModern drug development is about specificity.
- Enzymes facilitate many of the chemical reactions that are necessary for life: from digestion of nutrients to synthesis of DNA.
- Enzymes display a very high specificity-of-action, with any given enzyme generally recognizing only one or a handful of potential substrates.
- Inhibition of a specific enzyme allows a researcher to better understand a metabolic pathway, and opens up avenues for novel drug design
- Some inhibitors prevent enzymes from recognizing or binding to substrates, either by masking the substrate or by blocking the active-site on the enzyme. (Competitive inhibition).
- Alternatively, some enzyme inhibitors may significantly reduce enzymatic activity without affecting substrate recognition or binding. (Non-competitive inhibition)
- Some enzyme inhibitors are capable of affecting enzymes in a variety of different ways, and can provide a mixture of competitive and non-competitive inhibition (Mixed-inhibition)
Enzyme inhibitors may be reversible or irreversible
- Reversible enzyme inhibitors form a non-covalent bond with an enzyme. They may temporarily block or slow enzymatic function, but the effects are (by nature) reversible. Reversible enzyme inhibitors are typically easily removed by dilution or dialysis.
- Irreversible enzyme inhibitors form a covalent bond with an enzyme. They permanently alter the chemical structure of the enzyme thereby irreversibly slowing or blocking enzymatic function.
Enzyme Inhibitors ready for purchase
| Pathway | Inhibitors |
|---|---|
| ACAT Inhibitors | Pellitorine Terpendole C |
| ACC2 Inhibitors | ACC2 Inhibitor |
| Adenylase Cyclase Inhibitors | KH7 SQ 22536 |
| Aldo-Keto Reductase (AKR) Inhibitors | AKR1C3 Inhibitor I AKR1C3 Inhibitor II AKR1C3 Inhibitor III |
| Angiogenesis Inhibitors | 2-Methoxyestradiol BIBF1120 Borrelidin Castanospermine Fumagillin Isoxanthohumol Thiabendazole Tranilast |
| Angiotensin Receptor Antagonists | Valsartan |
| Arginase Inhibitors | BEC |
| ATPase Inhibitors | (-)-Blebbistatin Bafilomycin A1 Bufalin |
| Autophagy Inhibitors | 3-Methyladenine ATM Kinase Inhibitor, KU-55933 Bafilomycin A1 Chloroquine Diphosphate Go 6976 Spautin-1 |
| Bcl-2 Inhibitors | ABT-263 ABT-737 AT-101 BCl-2 Inhibitor GX15-070 BCl-2 Inhibitor, ABT-199 |
| BMP Inhibitors | EZSolutionTM LDN193189 LDN193189 |
| Bone Resorption Inhibitors | Alendronate sodium Pamidronate disodium |
| Bromodomain Inhibitors | (-)-JQ1 Bromodomain Inhibitor, (+)-JQ1 I-BET151 PFI-1 |
| Calpain Inhibitors | Calpain Inhibitor I, ALLN Calpain Inhibitor II, ALLM Calpain Inhibitor Z-LLY-FMK MDL 28170 PD 150,606 |
| Caspase & Granzyme B Inhibitors | Biotin-DEVD-FMK Biotin-IETD-FMK Biotin-VAD-FMK Caspase Inhibitor Boc-D-FMK Caspase-1 Inhibitor Z-YVAD-FMK Caspase-10 Inhibitor AEVD-FMK Caspase-12 Inhibitor Caspase-13 Inhibitor LEED-FMK Caspase-2 Inhibitor Z-VDVAD-FMK Caspase-3 Inhibitor Q-DEVD-OPh Caspase-3 Inhibitor Z-DEVD-FMK Caspase-4 Inhibitor Z-LEVD-FMK Caspase-5 Inhibitor Z-WEHD-FMK Caspase-6 Inhibitor Z-VEID-FMK Caspase-8 Inhibitor Z-IETD-FMK Caspase-8 Inhibitor, Q-IETD-OPh Caspase-9 Inhibitor Z-LEHD-FMK Caspase-9 Inhibitor, Q-LEHD-OPh EMAP-II Inhibitor Z-ASTD-FMK EZSolutionTM Q-VD-OPh, Negative Control FMK Negative Control Granzyme B Inhibitor Ac-IEPD-CHO Q-VD-OPh Z-ATAD-FMK Caspase-3 Inhibitor Z-DEVD-FMK Z-FA-FMK Caspase-8 Inhibitor Z-IETD-FMK Caspase-9 Inhibitor Z-LEHD-FMK Caspase-4 Inhibitor Z-LEVD-FMK Caspase-Family Inhibitor Z-VAD-FMK |
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