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107 results for "Active Degraders" in Products

Active Degraders Products

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 ...

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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

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

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

Potent and selective focal adhesion kinase (FAK) Degrader (PROTAC®)

Chemical Name: (2S,4R)-4-Hydroxy-1-((S)-2-(2-(4-(3-methoxy-4-((4-((2-(methylcarbamoyl)phenyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Potent and selective focal adhesion kinase (FAK) degrader

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 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®

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

(+)-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

(+)-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 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 EGFR PROTAC® Degrader

Alternate Names: Iressa-based PROTAC 3
Chemical Name: (2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)pentyl)oxy)ethoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Potent EGFR PROTAC®

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®)

Potent tropomyosin receptor kinase (TRK) Degrader

Chemical Name: 2-(2,6-Dioxo-3-piperidinyl)-4-[[2-[3-[4-[6-[6-[(2R)-2-(3-fluorophenyl)-1-pyrrolidinyl]imidazo[1,2-b]pyridazin-3-yl]-2-pyridinyl]-1-piperazinyl]-3-oxopropoxy]ethyl]amino]-1H-isoindole-1,3(2H)-dione
Purity: ≥98% (HPLC)
Potent tropomyosin receptor kinase (TRK) degrader

Degrader of MTH1 fusion proteins for use within the aTAG system

Alternate Names: CFT 2139
Chemical Name: 6-(6-((4-(2-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamido)butyl)carbamoyl)pyridin-3-yl)-N-methyl-4-(phenylamino)quinoline-3-carboxamide
Purity: ≥98% (HPLC)
Degrader of MTH1 fusion proteins for use within the aTAG system

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

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®)

PDEδ autophagy-tethering compound (ATTEC) Degrader

Chemical Name: N-(6-(2-(2,6-Dibromo-4-((5-iodo-2-oxoindolin-3-ylidene)methyl)phenoxy)acetamido)hexyl)-4-(3,4-dimethyl-7-oxo-2-(p-tolyl)-2,7-dihydro-6H-pyrazolo[3,4-d]pyridazin-6-yl)butanamide
Purity: ≥98% (HPLC)
PDEδ autophagy-tethering compound (ATTEC) Degrader

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

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

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®)

SARS-CoV-2 Mpro Degrader (PROTAC®)

Chemical Name: 3-((6-((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)hexyl)oxy)benzyl ((2S,3R)-3-(tert-butoxy)-1-(((S)-3-cyclohexyl-1-oxo-1-(((S)-1-oxo-3-((S)-2-oxopyrrolidin-3-yl)propan-2-yl)amino)propan-2-yl)amino)-1-oxobutan-2-yl)carbamate
Application of MPD 2
(2)

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®
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