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Active Degraders Products

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.

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107 results for "Active Degraders" in Products

107 results for "Active Degraders" in Products

Active Degraders Products

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.

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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)
Potent and selective degrader of mutant FKBP12F36V fusion proteins

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)
Degrades mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation

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)
Degrades mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation

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)
First generation Degrader for mutant FKBP12F36V fusion proteins; useful alternative to genetic methods for target validation

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)
Live-cell luminescent kinetic degradation assay
(2)

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)
Potent TANK-binding kinase 1 (TBK1) PROTAC®

(+)-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)
Application of MZ 1 in HeLa Cells
(2)

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 (+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo

(+)-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)
(+)-JQ1 based Degrader (PROTAC®) targeting BET bromodomains, active in vivo

Selective and potent TAG Degrader for auxin-inducible degron 2 system

Chemical Name: 5-Phenyl-1H-indole-3-acetic acid
Purity: ≥98% (HPLC)
Selective and potent TAG Degrader for auxin-inducible degron 2 system

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 and selective p38α and p38β Degrader (PROTAC®); active in vivo

Potent tropomyosin receptor kinase (TRK) Degrader

Chemical Name: 2-(2,6-Dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]-1H-isoindole-1,3(2H)-dione
Purity: ≥98% (HPLC)
Potent tropomyosin receptor kinase (TRK) degrader

Cereblon Degrader (PROTAC®)

Chemical Name: N1-(2-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)-N20-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-3,9,12,18-tetraoxaicosanediamide
Purity: ≥98% (HPLC)
Cereblon Degrader (PROTAC®)

PDEδ autophagy-tethering compound (ATTEC) Degrader

Chemical Name: N-(6-(2-(2,6-Dibromo-4-((5-iodo-2-oxoindolin-3-ylidene)methyl)phenoxy)acetamido)hexyl)-4-(3,4-dimethyl-7-oxo-2-(p-tolyl)-2,7-dihydro-6H-pyrazolo[3,4-d]pyridazin-6-yl)butanamide
Purity: ≥98% (HPLC)
PDEδ autophagy-tethering compound (ATTEC) Degrader

Homo-PROTAC® for self-degradation of pVHL30

Chemical Name: N1,N20-bis((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-3,6,9,12,15,18-hexaoxaicosanediamide
Purity: ≥98% (HPLC)
Homo-PROTAC® for self-degradation of pVHL30

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 of MTH1 fusion proteins for use within the aTAG system

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)
α-synuclein PROTAC® Degrader

(+)-JQ1 based PROTAC® with selectivity for BRD4

Chemical Name: (2S,4R)-1-(2R)-2-Acetamido-3-[[6-[2-[(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]acetamido]hexyl]thio]-3-methylbutanoyl]-4-hydroxy-N-[4-(4-methylthiazol-5-yl)benzyl)pyrrolidinine-2-carboxamide
Purity: ≥98% (HPLC)
(+)-JQ1 based PROTAC® with selectivity for BRD4

Potent EGFR PROTAC® Degrader

Alternate Names: Iressa-based PROTAC 3
Chemical Name: (2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)pentyl)oxy)ethoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Potent EGFR PROTAC®

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)
Degrader of MTH1 fusion proteins for use within the aTAG system

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 BRD9 Degrader (PROTAC®)

PRC1 Degrader (PROTAC®); degrades BMI1 and RING1B

Chemical Name: (2S,4R)-1-((S)-2-(7-(5-(4-(4-(5-((Furan-2-ylmethyl)amino)-[1,2,4]triazolo[4,3-c]pyrimidin-8-yl)phenyl)piperazin-1-yl)pentanamido)heptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride
Purity: ≥97% (HPLC)
PRC1 Degrader (PROTAC®); degrades BMI1 and RING1B

Potent PARP1 Degrader (PROTAC®)

Chemical Name: N-(2-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)-12-(4-(2-fluoro-5-((4-oxo-3,4-dihydrophthalazin-1-yl)methyl)benzoyl)piperazin-1-yl)-12-oxododecanamide
Purity: ≥98% (HPLC)
Potent PARP1 Degrader (PROTAC®)

Selective peptide-based β-catenin Degrader (PROTAC®)

Purity: ≥95% (HPLC)
Selective peptide-based β-catenin Degrader (PROTAC®)

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 CDK2 degrader (PROTAC®)
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