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107 results for "Active Degraders" in Products

Active Degraders 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)
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

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

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

(+)-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 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)
Potent and selective Wee1 Degrader (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®)

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

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

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

(+)-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

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)

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 (+)-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

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 KRAS PROTAC®

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)
Potent MIF Degrader (PROTAC®)

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% (HPLC)
Potent and selective EP300 Degrader

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% (HPLC)
Potent and selective androgen receptor PROTAC®

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®

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% (HPLC)
Potent BRD9 Degrader (PROTAC®)

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% (HPLC)
Potent EGFR PROTAC®; also degrades HER2

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% (HPLC)
Potent and selective BTK Degrader (PROTAC®)

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)
Application of CRBN-6-5-5-VHL in MM1S cells for CRBN-6-5-5-VHL
(2)

JQ1-maleimide functionalized probe; induces proteasomal degradation of BRD4

Chemical Name: (S)-N-(2-(2-(2-(2-(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)ethoxy)ethoxy)ethyl)-6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamide
Purity: ≥95% (HPLC)
JQ1-maleimide functionalized probe; induces proteasomal degradation of BRD4

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)
Potent and selective ERK5 Degrader (PROTAC®)
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