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109 results for "Active Degraders" in Products

Active Degraders Products

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 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

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®

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

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 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

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

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

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

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)
Selective and potent TAG Degrader for auxin-inducible degron 2 system; 5-Ph-IAA analog

Selective EGFR PROTAC® Degrader

Chemical Name: (2S,4R)-1-((S)-2-(tert-Butyl)-14-(4-(4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6-yl)phenoxy)-4-oxo-6,9,12-trioxa-3-azatetradecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Selective EGFR PROTAC®

Potent and selective HDAC4 Degrader (PROTAC®)

Chemical Name: (2S,4R)-1-((3R,26S)-26-(tert-Butyl)-3-methyl-1,24-dioxo-5-propyl-1-(4-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)phenyl)-10,13,16,19,22-pentaoxa-2,5,25-triazaheptacosan-27-oyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Potent and selective HDAC4 Degrader (PROTAC®)

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 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 GSK3 Degrader (PROTAC®)

Chemical Name: 3-Amino-6-(4-((4-(4-(1-(17-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)-3,6,9,12,15-pentaoxaheptadecyl)-1H-1,2,3-triazol-4-yl)butyl)piperazin-1-yl)sulfonyl)phenyl)-N-(pyridin-3-yl)pyrazine-2-carboxamide
Purity: ≥98% (HPLC)
Potent GSK3 Degrader (PROTAC®)

Selective Cdk4/6 Degrader (PROTAC®

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)
Selective Cdk4/6 Degrader (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)

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

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)
SNAP tag labeled fusion protein Degrader (PROTAC®)

Potent pan IAP Degrader (PROTAC®)

Chemical Name: (2S,4S)-1-((S)-2-Cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)-4-(3-((5-(((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)-5-oxopentyl)oxy)phenoxy)-N-((R)-1,2,3,4-tetrahydronaphthalen-1-yl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
IAP-VHL Degrader

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

Cyclin D1, CDK4/6 and cyclin D3 Degrader (PROTAC®)

Chemical Name: (2S,4R)-1-((S)-2-(7-(4-(6-((6-Acetyl-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazin-1-yl)-7-oxoheptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Cyclin D1, CDK4/6 and cyclin D3 Degrader (PROTAC&reg:)

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®)
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