107 results for "Active Degraders" in Products
Active Degraders
Protein Degraders (e.g.PROTAC® molecules, SNIPERs etc), are a useful approach for the knockdown of target proteins within cells. Comprising 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 and can be used to investigate downstream effects of protein knockdown or to interfere with specific signaling pathways. The methodology provides an attractive alternative to ...
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% |
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% |
Selective and potent TAG Degrader for auxin-inducible degron 2 system
| Chemical Name: | 5-Phenyl-1H-indole-3-acetic acid |
| Purity: | ≥98% |
(+)-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% |
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% |
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% |
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% |
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% |
Selective peptide-based β-catenin Degrader (PROTAC®)
| Purity: | ≥95% |
(+)-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% |
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% |
Potent BRD9 Degrader (PROTAC®)
| Chemical Name: | 2-((2,6-Dimethoxy-4-(2-methyl-1-oxo-1,2-dihydro-2,7-naphthyridin-4-yl)benzyl)(methyl)amino)-N-(8-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)octyl)acetamide |
| Purity: | ≥98% |
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% |
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% |
Potent and selective BTK Degrader (PROTAC®)
| Chemical Name: | 4-(1,1-Dimethylethyl)-N-[3-[6-[[4-[[4-[6-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]acetyl]amino]hexyl]-1-piperazinyl]carbonyl]phenyl]amino]-4,5-dihydro-4-methyl-5-oxo-2-pyrazinyl]-2-methylphenyl]benzamide |
| Purity: | ≥98% |
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% |
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% |
Potent EGFR PROTAC® Degrader; also degrades HER2
| Chemical Name: | (2S,4R)-1-((S)-2-(2-(2-(2-(4-(4-((3-Chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6- yl)phenoxy)ethoxy)ethoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% |
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% |
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% |
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% |
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% |
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% |
(+)-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% |
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% |
