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.
Products:
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.
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) |
(+)-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) |
(+)-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) |
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) |
Selective and potent TAG Degrader for auxin-inducible degron 2 system
| Chemical Name: | 5-Phenyl-1H-indole-3-acetic acid |
| 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 ERK5 Degrader (PROTAC®)
| Chemical Name: | (2S,4R)-1-((S)-2-(7-(4-(4-((5,11-Dimethyl-6-oxo-6,11-dihydro-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-2-yl)amino)-3-methoxyphenyl)piperazin-1-yl)heptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% (HPLC) |
Selective HDAC3 Degrader (PROTAC®)
| Chemical Name: | (2S,4R)-N-[2-[[12-[[4-[(2-Aminophenyl)carbamoyl]phenyl]amino]-12-oxododecyl]oxy]-4-(4-methylthiazol-5-yl)benzyl]-1-[(S)-2-(1-fluorocyclopropan-1-ylcarbonylamino)-3,3-dimethylbutanoyl]-4-hydroxypyrrolidine-2-carboxamide |
| 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) |
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) |
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) |
Selective and potent TAG Degrader for auxin-inducible degron 2 system; 5-Ph-IAA analog
| Chemical Name: | Acetoxymethyl 2-(5-phenyl-1H-indol-3-yl)acetate |
| Purity: | ≥98% (HPLC) |
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) |
Potent and selective BRD7/9 Degrader (PROTAC®)
| Chemical Name: | (2S,4R)-N-(2-((5-(4-(2,6-Dimethoxy-4-(2-methyl-1-oxo-1,2-dihydro-2,7-naphthyridin-4-yl)benzyl)piperazin-1-yl)pentyl)oxy)-4-(4-methylthiazol-5-yl)benzyl)-1-((S)-2-(1-fluorocyclopropane-1-carboxamido)-3,3-dimethylbutanoyl)-4-hydroxypyrrolidine-2-carboxamide |
| Purity: | ≥98% (HPLC) |
Selective α1A adrenergic receptor Degrader (PROTAC®)
| Chemical Name: | 2-(2-(2-(2-(4-(4-(4-Amino-6,7-dimethoxyquinazolin-2-yl)piperazine-1-carbonyl)-1H-1,2,3-triazol-1-yl)ethoxy)ethoxy)ethoxy)-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)acetamide |
| 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) |
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) |
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 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) |
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) |
Potent hematopoietic prostaglandin D2 synthase Degrader (PROTAC®)
| Chemical Name: | N-[4-[4-[[4-[2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]-1-piperazinyl]carbonyl]-1-piperidinyl]phenyl]-2-phenoxy-5-pyrimidinecarboxamide |
| 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 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) |
CDK6 and CDK4 HSP90-mediated targeting chimera (HEMTAC) Degrader
| Chemical Name: | 4-[6-[(6-Acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-N-[[1-[4-[2-amino-4-chloro-7-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-3-butyn-1-yl]-1H-1,2,3-triazol-4-yl]methyl]-1-piperazineacetamide |
| Purity: | ≥95% (HPLC) |
