Description: Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.
MCE covalent inhibitor library contains 2988 small molecules including identified covalent inhibitors and other molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.
MCE Covalent inhibitor Library plus, with more powerful screening capability, further complement Covalent inhibitor Library (HY-L036) by adding some fragment compounds with covalent warheads.
MCE Covalent Screening Library Plus can be supplied as pre-dissolved Solutions or Solid. For pre-dissolved solutions in this library, there are 2953 compounds supplied in 10 mM solution, 23 compounds supplied in 2 mM solution and 2 compounds supplied in 3 mg/mL solution.
For pre-dissolved solutions, 10 mM for compounds with the solubility not lower than 10 mM, 2 mM for compounds with solubility between 2 mM and 10 mM, and 3 mg/mL for compounds with unconfirmed molecular weight and solubility not lower than 3 mg/mL.
Advantages:
- A unique collection of 2988 compounds that show irreversible covalent binding with target proteins for high throughput screening (HTS) and high content screening (HCS).
- Chemical probes that show enhanced selectivity, potency and utility for biological studies.
- A useful tool for drug discovery with irreversible inhibition.
- Structurally diverse, medicinally active, and cell permeable.
- Detailed compound information with structure, IC50, and brief introduction.
- Validated NMR and HPLC to ensure high purity and quality.
- All compounds are in stock and continuously updated.
Formulation: A collection of 2988 molecules supplied as pre-dissolved Solutions or SolidSolution:2953 compounds supplied in 10 mM solution,23 compounds supplied in 2 mM solution,2 compounds supplied in 3 mg/mL solution.
Layout: 96-well storage tube or 96-well plate: 1st and 12th column are left empty.384-well plate: the first two columns and the last two columns are left empty.Compounds with different concentrations or dissolved in different solvents will be put on separate plates.This way of layout may increase the number of plates because there could be three solvents and three concentrations. If you have other requirements, please let us know.
Container: 96- or 384-well Plate with Peelable Foil Seal
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