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44 results for "active degraders" in Products

44 results for "active degraders" in Products

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)
TAG Degradation Platforms Small Molecule

(+)-JQ1 based Degrader (PROTAC®) that selectively 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)
Active Degraders Small Molecule

Potent and selective degrader of mutant FKBP12F36V fusion proteins

Catalog #: 6914
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)
TAG Degradation Platforms Small Molecule

Potent and selective androgen receptor PROTAC®

Catalog #: 7254
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)
Active Degraders Small Molecule

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

Catalog #: 6912
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)
TAG Degradation Platforms Small Molecule

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

Catalog #: 6356
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)
Active Degraders Small Molecule

Fluorescent HIF-1α peptide; can be used to evaluate the effect of VHL binding on degradation activity

Catalog #: 7287
Purity : ≥95% (HPLC)
Other Fluorescent Probes Peptide

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

Catalog #: 6945
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)
Active Degraders Small Molecule

Multikinase Degrader (PROTAC®)

Catalog #: 6524
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)
Active Degraders Small Molecule

Potent TANK-binding kinase 1 (TBK1) PROTAC®

Catalog #: 7259
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)
Active Degraders Small Molecule

Cereblon Degrader (PROTAC®)

Catalog #: 7219
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)
Active Degraders Small Molecule

Potent and selective p38α PROTAC®

Catalog #: 7268
Alternate Names : SJFa PROTAC, SJFalpha PROTAC, SJFα PROTAC
Chemical Name : N-(3-Fluoro-4-((7-(4-(4-(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)butoxy)butoxy)-6-methoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Purity : ≥98% (HPLC)
Active Degraders Small Molecule

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

Catalog #: 6327
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)
Active Degraders Small Molecule

Potent and selective cereblon Degrader (PROTAC®); cell-permeable

Catalog #: 6948
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)
Active Degraders Small Molecule

Potent and selective Cdk9 Degrader (PROTAC®)

Chemical Name : N-(5-(((5-(tert-Butyl)oxazol-2-yl)methyl)thio)thiazol-2-yl)-1-(14-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-2-oxo-6,9,12-trioxa-3-azatetradecyl)piperidine-4-carboxamide
Purity : ≥98% (HPLC)
Cyclin-dependent Kinase Inhibitors Small Molecule

Hydrochloride salt of dTAGV-1 (Cat. No. 6914); suitable for in vivo use

Catalog #: 7374
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)
TAG Degradation Platforms Small Molecule

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

Catalog #: 7177
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)
Active Degraders Small Molecule

Potent and selective BTK Degrader (PROTAC®)

Catalog #: 7160
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% (HPLC)
Active Degraders Small Molecule

Selective Cdk4/6 Degrader (PROTAC®)

Catalog #: 6938
Chemical Name : N-[4-[4-[6-[(6-Acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-1-piperazinyl]butyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetamide
Purity : ≥98% (HPLC)
Active Degraders Small Molecule

Selective Cdk6 Degrader (PROTAC®)

Catalog #: 6921
Chemical Name : N-[2-[2-[2-[2-[4-[6-[(6-Acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-1-piperazinyl]ethoxy]ethoxy]ethoxy]ethyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetamide
Purity : ≥98% (HPLC)
Active Degraders Small Molecule

SRC-1 peptide-based PROTAC®; active in vivo

Catalog #: 7388
Purity : ≥95% (HPLC)
Active Degraders Peptide

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)
Active Degraders Small Molecule

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

Catalog #: 7298
Purity : ≥95% (HPLC)
Active Degraders Peptide

Homo-PROTAC for self-degradation of pVHL30

Catalog #: 6416
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)
Active Degraders Small Molecule

Photoswitchable BET bromodomain Degrader (PHOTAC)

Catalog #: 7319
Chemical Name : 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)-N-(4-(2-(4-((E)-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)diazenyl)-2,6-dimethoxyphenoxy)acetamido)butyl)acetamide
Purity : ≥98% (HPLC)
Active Degraders Small Molecule
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