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:
104 results for "Active Degraders Small Molecules and Peptides" in Products
104 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) |
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 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) |
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) |
Hydrochloride salt of dTAGV-1 (Cat. No. 6914); suitable for in vivo use
| 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 hydrochloride |
| 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) |
(+)-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 MIF Degrader (PROTAC®)
| Chemical Name: | 8-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-N-(4-(7-hydroxy-2-oxo-2H-benzo[e][1,3]oxazin-3(4H)-yl)phenyl)octanamide |
| Purity: | ≥98% (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) |
CDK8 Degrader (PROTAC®)
| Chemical Name: | 15-[[2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]-N-[(3β,5α,17β)-17-(7-isoquinolinyl)androstan-3-yl]-N-methyl-4,7,10,13-tetraoxapentadecanamide |
| Purity: | ≥98% (HPLC) |
Potent and selective cereblon Degrader (PROTAC®); cell-permeable
| Chemical Name: | (2S,4R)-1-((2S)-2-(5-((5-((6-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)hexyl)oxy)pentyl)oxy)pentanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥96% (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) |
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) |
Degrader (PROTAC®) of SNAP-tag™ labeled fusion proteins
| Chemical Name: | N-(4-(((2-Amino-6-chloropyrimidin-4-yl)oxy)methyl)benzyl)-2-(1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)piperidin-4-yl)acetamide |
| Purity: | ≥97% (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) |
SRC-1 peptide-based Degrader (PROTAC®); active in vivo
| Purity: | ≥95% (HPLC) |
Degrader (PROTAC®) of SNAP-tag™ labeled fusion proteins
| Chemical Name: | N1-(4-(((2-Amino-6-chloropyrimidin-4-yl)oxy)methyl)benzyl)-N7-((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)heptanediamide |
| Purity: | ≥98% (HPLC) |
Potent and selective BRD9 Degrader (PROTAC®)
| Chemical Name: | 2-[[[4-(1,2-Dihydro-2-methyl-1-oxo-2,7-naphthyridin-4-yl)-2-6-dimethoxyphenyl]methyl]methylamino]-N-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethyl]acetamide dihydrochloride |
| Purity: | ≥98% (HPLC) |
Potent and selective USP7 Degrader (PROTAC®)
| Chemical Name: | 3-(1-(1-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)piperidine-4-carbonyl)piperidin-4-yl)-N-(3-((4-hydroxy-1-((R)-3-phenylbutanoyl)piperidin-4-yl)methyl)-4-oxo-3,4-dihydroquinazolin-7-yl)propanamide |
| Purity: | ≥96% (HPLC) |
Selective Cdk4 Degrader (PROTAC®)
| Chemical Name: | 7-Cyclopentyl-2-[[5-[4-[4-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl]oxy]acetamido]butyl]piperazin-1-yl]pyridin-2-yl]amino]-N,N-dimethyl-7H-pyrrolo[2,3d]pyrimidine-6-carboxamide |
| Purity: | ≥98% (HPLC) |
First generation Degrader for mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation
| Chemical Name: | (1R)-3-(3,4-Dimethoxyphenyl)-1-(2-((19-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)-2,18-dioxo-7,10,13-trioxa-3,17-diazanonadecyl)oxy)phenyl)propyl (2S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate |
| Purity: | ≥98% (HPLC) |
c-MET PROTAC®; also degrades exon-14-deleted c-MET
| Chemical Name: | N-(3-Fluoro-4-((7-(3-(3-(3-(((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)-3-oxopropoxy)propoxy)propoxy)-6-methoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
| Purity: | ≥98% (HPLC) |
Degrader of MTH1 fusion proteins for use within the aTAG system
| Alternate Names: | CFT 4531 |
| Chemical Name: | N-Cyclopropyl-6-(4-((4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)methyl)-1H-1,2,3-triazol-1-yl)butyl)carbamoyl)-3-fluorophenyl)-7-fluoro-4-(phenylamino)quinoline-3-carboxamide |
| Purity: | ≥98% (HPLC) |
