Active Degraders: Small Molecules and Peptides

dTAG^V-1

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)

dTAG-13

Catalog #: 6605

(4)

Citations (136)

Product Documents

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)

BromoTag^® AGB1

Catalog #: 7686

Citations (12)

Product Documents

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)

dTAG^V-1 hydrochloride

Catalog #: 7374

(1)

Citations (3)

Product Documents

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)

dBET6

Catalog #: 6945

Citations (8)

Product Documents

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)

dTAG-47

Catalog #: 7530

Citations (4)

Product Documents

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)

PDEδ ATTEC 12C

Catalog #: 8824

Product Documents

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)

NR 7h

Catalog #: 7177

Citations (1)

Product Documents

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)

dBET1

Catalog #: 6327

Citations (3)

Product Documents

(+)-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)

LC 2

Catalog #: 7420

Citations (1)

Product Documents

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)

dTAG-7

Catalog #: 6912

Citations (10)

Product Documents

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)

CM 11

Catalog #: 6416

Citations (1)

Product Documents

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)

BromoTag^® AGB3

Catalog #: 7688

Product Documents

Selective Degrader of Brd4BD2 L387A fusion proteins (BromoTag®)

Chemical Name:	(2S,4R)-1-((2S,17R)-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-diazanonadecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity:	≥98% (HPLC)

MS 147

Catalog #: 8077

Product Documents

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)

5-Ph-IAA-AM

Catalog #: 7893

Citations (1)

Product Documents

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)

TBK1 PROTAC^® 3i

Catalog #: 7259

Citations (3)

Product Documents

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)

BSJ-03-123

Catalog #: 6921

Citations (2)

Product Documents

Selective Cdk6 Degrader (PROTAC®)

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)

MZ 1

Catalog #: 6154

Citations (18)

Product Documents

(+)-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)

HDAC4 CHDI Degrader 11

Catalog #: 7882

Product Documents

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)

AUTAC4

Catalog #: 7699

Product Documents

Mitochondrial targeting AUTAC Degrader

Chemical Name:	N-[(16R)-16-[[[2-Amino-9-[(4-fluorophenyl)methyl]-6,9-dihydro-6-oxo-1H-purin-8-yl]thio]methyl]-15,18-dioxo-4,7,10-trioxa-14,17-diazanonadec-1-yl]-α-oxo-2-phenyl-1H-indole-3-acetamide
Purity:	≥98% (HPLC)

JPS036

Catalog #: 8085

Product Documents

Selective HDAC3 Degrader (PROTAC®)

Chemical Name:	(2S,4R)-N-[2-[[12-[[4-[(2-Aminophenyl)carbamoyl]phenyl]amino]-12-oxododecyl]oxy]-4-(4-methylthiazol-5-yl)benzyl]-1-[(S)-2-(1-fluorocyclopropan-1-ylcarbonylamino)-3,3-dimethylbutanoyl]-4-hydroxypyrrolidine-2-carboxamide
Purity:	≥98% (HPLC)

PT-65

Catalog #: 7651

Citations (1)

Product Documents

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)

SJF 1521

Catalog #: 7261

Citations (1)

Product Documents

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)

CG 428

Catalog #: 7425

Citations (1)

Product Documents

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)

VHL-SNAP2-5C

Catalog #: 8890

Product Documents

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)

Active Degraders: Small Molecules and Peptides

dTAG^V-1

dTAG-13

BromoTag^® AGB1

dTAG^V-1 hydrochloride

dBET6

dTAG-47

PDEδ ATTEC 12C

NR 7h

dBET1

LC 2

dTAG-7

CM 11

BromoTag^® AGB3

MS 147

5-Ph-IAA-AM

TBK1 PROTAC^® 3i

BSJ-03-123

MZ 1

HDAC4 CHDI Degrader 11

AUTAC4

JPS036

PT-65

SJF 1521

CG 428

VHL-SNAP2-5C

CONTACT INFORMATION

保持关注

Active Degraders: Small Molecules and Peptides

dTAGV-1

dTAG-13

BromoTag® AGB1

dTAGV-1 hydrochloride

dBET6

dTAG-47

PDEδ ATTEC 12C

NR 7h

dBET1

LC 2

dTAG-7

CM 11

BromoTag® AGB3

MS 147

5-Ph-IAA-AM

TBK1 PROTAC® 3i

BSJ-03-123

MZ 1

HDAC4 CHDI Degrader 11

AUTAC4

JPS036

PT-65

SJF 1521

CG 428

VHL-SNAP2-5C

dTAG^V-1

BromoTag^® AGB1

dTAG^V-1 hydrochloride

BromoTag^® AGB3

TBK1 PROTAC^® 3i