Active Degraders: Small Molecules and Peptides
Degraders are a way to knock down target proteins within cells. They are made up of binding moieties for an E3 ubiquitin ligase and a target protein joined by a linker. These hybrid molecules induce selective, proteasome-dependent degradation of target proteins. Degraders be also used to investigate the downstream effects of protein knockdown or to interfere with specific signaling pathways.
Products:
108 results for "Active Degraders Small Molecules and Peptides" in Products
108 results for "Active Degraders Small Molecules and Peptides" in Products
Active Degraders: Small Molecules and Peptides
Degraders are a way to knock down target proteins within cells. They are made up of binding moieties for an E3 ubiquitin ligase and a target protein joined by a linker. These hybrid molecules induce selective, proteasome-dependent degradation of target proteins. Degraders be also used to investigate the downstream effects of protein knockdown or to interfere with specific signaling pathways.
Products:
Potent and selective degrader of mutant FKBP12F36V fusion proteins
| Chemical Name: | (R)-3-(3,4-Dimethoxyphenyl)-1-(2-(2-((7-(((S)-1-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-7-oxoheptyl)amino)-2-oxoethoxy)phenyl)propyl (S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate trifluoroacetate |
| Purity: | ≥98% (HPLC) |
Degrades mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation
| Chemical Name: | 1-[(2S)-1-Oxo-2-(3,4,5-trimethoxyphenyl)butyl]-(2S)-2-piperidinecarboxylate (1R)-3-(3,4-dimethoxyphenyl)-1-[2-[2-[[6-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]hexyl]amino]-2-oxoethoxy]phenyl]propyl ester |
| Purity: | ≥98% (HPLC) |
α-synuclein Degrader (PROTAC®)
| Chemical Name: | 2-[[3-[5-(1,3-Benzodioxol-5-yl)-1H-pyrazol-3-yl]phenyl]amino]-N-[2-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethyl]acetamide |
| Purity: | ≥98% (HPLC) |
Degrades mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation
| Chemical Name: | (1R)-3-(3,4-Dimethoxyphenyl)-1-(2-(2-((8-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)octyl)amino)-2-oxoethoxy)phenyl)propyl (2S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate |
| Purity: | ≥97% (HPLC) |
Potent and selective CDK2 Degrader (PROTAC®)
| Chemical Name: | 4-[[5-Amino-1-[(3-methyl-2-thienyl)carbonyl]-1H-1,2,4-triazol-3-yl]amino]-N-[2-[[1-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethyl]-1H-1,2,3-triazol-4-yl]methoxy]ethyl]benzenesulfonamide |
| Purity: | ≥98% (HPLC) |
Selective and potent TAG Degrader for auxin-inducible degron 2 system
| Chemical Name: | 5-Phenyl-1H-indole-3-acetic acid |
| Purity: | ≥98% (HPLC) |
Potent and selective (+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo
| Chemical Name: | (6S)-4-(4-Chlorophenyl)-N-[8-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]octyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide |
| Purity: | ≥98% (HPLC) |
Potent and selective p38α and p38β Degrader (PROTAC®); active in vivo
| Chemical Name: | 3-(3-Bromo-4-((2,4-difluorobenzyl)oxy)-6-methyl-2-oxopyridin-1(2H)-yl)-N-(4-(1-(4-((4-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)butyl)amino)-4-oxobutyl)-1H-1,2,3-triazol-4-yl)butyl)-4-methylbenzamide |
| Purity: | ≥97% (HPLC) |
Potent TANK-binding kinase 1 (TBK1) PROTAC®
| Chemical Name: | (2S,4R)-1-((S)-18-(4-((5-Bromo-4-((3-(N-methylcyclobutanecarboxamido)propyl)amino)pyrimidin-2-yl)amino)phenoxy)-2-(tert-butyl)-4-oxo-6,10,15-trioxa-3-azaoctadecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% (HPLC) |
SRC-1 peptide-based Degrader (PROTAC®); active in vivo
| Purity: | ≥95% (HPLC) |
Selective peptide-based β-catenin Degrader (PROTAC®)
| Purity: | ≥95% (HPLC) |
(+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo
| Chemical Name: | (6S)-4-(4-Chlorophenyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide |
| Purity: | ≥98% (HPLC) |
Potent and selective Wee1 Degrader (PROTAC®)
| Chemical Name: | 4-((3-(4-(4-((2-Allyl-1-(6-(2-hydroxypropan-2-yl)pyridin-2-yl)-3-oxo-2,3-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6-yl)amino)phenyl)piperazin-1-yl)propyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione |
| Purity: | ≥98% (HPLC) |
Potent and selective trivalent BET Bromodomain Degrader (PROTAC®)
| Chemical Name: | N,N'-(11-((2-(((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)methyl)-11-methyl-3,6,9,13,16,19-hexaoxahenicosane-1,21-diyl)bis(2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide) |
| Purity: | ≥98% (HPLC) |
Potent and selective androgen receptor Degrader (PROTAC®)
| Chemical Name: | (2S,4R)-1-((S)-2-(2-(4-((4'-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-[1,1'-biphenyl]-4-yl)oxy)butoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% (HPLC) |
Potent and selective EP300 Degrader (PROTAC®)
| Chemical Name: | 12-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)-N-((R)-3'-(2-((4-fluorobenzyl)((S)-1,1,1-trifluoropropan-2-yl)amino)-2-oxoethyl)-2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-oxazolidin]-5-yl)dodecanamide |
| Purity: | ≥98% (HPLC) |
Potent and selective BTK Degrader (PROTAC®)
| Chemical Name: | 3-[[4-[1-[[1-[6-[[[(3S)-2,6-Dioxo-3-piperidinyl]amino]carbonyl]-3-pyridinyl]-4-piperidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-[(3R)-3-(3-methyl-2-oxo-1-imidazolidinyl)-1-piperidinyl]-2-pyrazinecarboxamide |
| Purity: | ≥98% (HPLC) |
Selective KRAS Degrader (PROTAC®)
| Chemical Name: | (2S,4R)-1-((S)-2-(3-(3-((S)-2-(((7-(8-Chloronaphthalen-1-yl)-4-((S)-3-(cyanomethyl)-4-(2-fluoroacryloyl)piperazin-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)oxy)methyl)pyrrolidin-1-yl)propoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥95% (HPLC) |
Potent and selective Degrader of Brd4BD2 L387A fusion proteins (BromoTag®)
| Chemical Name: | (S)-13-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidine-1-carbonyl)-14,14-dimethyl-11-oxo-3,6,9-trioxa-12-azapentadecyl (R)-2-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)butanoate |
| Purity: | ≥98% (HPLC) |
Multikinase Degrader (PROTAC®)
| Chemical Name: | N-(2-(2-(2-(4-(4-((5-Chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)phenyl)piperazin-1-yl)ethoxy)ethoxy)ethyl)-2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)acetamide |
| Purity: | ≥98% (HPLC) |
Potent and selective VHL-recruiting Degrader (PROTAC®) of mutant EGFR
| Chemical Name: | (2S,4R)-1-((S)-2-(11-(4-(3-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propyl)piperazin-1-yl)-11-oxoundecanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% (HPLC) |
Degrader of MTH1 fusion proteins for use within the aTAG system
| Alternate Names: | CFT 2139 |
| Chemical Name: | 6-(6-((4-(2-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamido)butyl)carbamoyl)pyridin-3-yl)-N-methyl-4-(phenylamino)quinoline-3-carboxamide |
| Purity: | ≥98% (HPLC) |
(+)-JQ1 based Degrader (PROTAC®) that preferentially degrades BRD4
| Chemical Name: | (2S,4R)-1-((S)-2-(tert-butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazaheptadecanoyl)- 4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% (HPLC) |
Potent and selective HER2 targeting Degrader (PROTAC®)
| Chemical Name: | 5-((7-(4-(3-((4-((4-([1,2,4]Triazolo[1,5-a]pyridin-7-yloxy)-3-methylphenyl)amino)-6-methoxyquinazolin-7-yl)oxy)propyl)piperazin-1-yl)heptyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione |
| Purity: | ≥98% (HPLC) |
Potent and selective nicotinamide phosphoribosyl transferase (NAMPT) Degrader (PROTAC®)
| Chemical Name: | (2S,4R)-1-((S)-18-(tert-Butyl)-1,16-dioxo-1-(4-((4-((4-(3-(pyridin-3-ylmethyl)thioureido)phenyl)sulfonyl)piperazin-1-yl)methyl)phenyl)-5,8,11,14-tetraoxa-2,17-diazanonadecan-19-oyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% (HPLC) |
