Bromodomain Inhibitors Small Molecules and Peptides

(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%

I-BET 151 dihydrochloride

Catalog #: 4650

(2)

Citations (10)

Product Documents

Images (1)

BET bromodomain inhibitor; also promotes differentiation of hiPSCs into megakaryocytes

Chemical Name:

7-(3,5-Dimethyl-4-isoxazolyl)-1,3-dihydroxy-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-2H-imidazo[4,5-c]quinolin-2-one dihydrochloride

Purity:

≥98%

dBRD9

Catalog #: 6606

Citations (12)

Product Documents

Images (1)

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%

XMD 8-92

Catalog #: 4132

Citations (13)

Product Documents

Images (1)

ERK5/BMK1 inhibitor; also BRD4 inhibitor

Chemical Name:

2-[[2-Ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one

Purity:

≥98%

I-BRD9

Catalog #: 5591

Citations (11)

Product Documents

Images (1)

Potent and selective BRD9 inhibitor

Chemical Name:

5-Ethyl-4,5-dihydro-4-oxo-N-(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)-7-[3-(trifluoromethyl)phenyl]thieno[3,2-c]pyridine-2-carboximidamide

Purity:

≥98%

cis MZ 1

Catalog #: 6155

Citations (1)

Product Documents

Images (1)

Negative Control for MZ 1 (Cat. No. 6154)

Chemical Name:

(2S,4S)-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%

dBET1

Catalog #: 6327

Citations (4)

Product Documents

Images (1)

(+)-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%

dBRD9-A

Catalog #: 6943

Citations (5)

Product Documents

Images (1)

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%

dBET6

Catalog #: 6945

Citations (8)

Product Documents

Images (1)

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%

PFI 1

Catalog #: 4445

Citations (5)

Product Documents

Images (1)

BET bromodomain inhibitor

Chemical Name:

2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide

Purity:

≥98%

Bromosporine

Catalog #: 4758

Citations (3)

Product Documents

Images (1)

Broad spectrum bromodomain inhibitor

Chemical Name:

N-[(6-3-Methanesulfonamido-4-methylphenyl)-3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-8-yl]carbamate

Purity:

≥98%

SGC-CBP30

Catalog #: 4889

(1)

Citations (13)

Product Documents

Images (1)

Potent CBP/p300 BRD inhibitor

Chemical Name:

2-[2-(3-Chloro-4-methoxyphenyl)ethyl]-5-(dimethyl-1,2-oxazol-4-yl)-1-[(2S)-2-(morpholin-4-yl)propyl]-1H-1,3-benzodiazole

Purity:

≥98%

PFI 3

Catalog #: 5072

Citations (7)

Product Documents

Images (1)

Potent and selective SMARCA2/4 and polybromo 1 inhibitor

Chemical Name:

(2E)-1-(2-Hydroxyphenyl)-3-[(1R,4R)-5-(pyridin-2-yl)-2,5-diazabicyclo[2.2.1]heptan-2-yl]prop-2-en-1-one

Purity:

≥98%

BAZ2-ICR

Catalog #: 5266

Citations (2)

Product Documents

Images (1)

Selective BAZ2 inhibitor

Chemical Name:

4-[4-(1-Methyl-1H-pyrazole-4-yl)-1-[2-(1-methyl-1H-pyrazol-4-yl)ethyl]-1H-imidazol-5-yl]benzonitrile

Purity:

≥98%

CPI 203

Catalog #: 5331

(1)

Citations (3)

Product Documents

Images (1)

BET bromodomain inhibitor; arrests cell cycle at G1 phase

Alternate Names:

TEN 010

Chemical Name:

(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide

Purity:

≥98%

NI 57

Catalog #: 5546

Citations (1)

Product Documents

Images (1)

Potent and selective BRPF bromodomain inhibitor

Chemical Name:

4-Cyano-N-(1,3-dimethyl-2-oxo-1,2-dihydroquinolin-6-yl)-2-methoxybenzene-1-sulfonamide

Purity:

≥98%

BI 9564

Catalog #: 5590

Citations (6)

Product Documents

Images (1)

Potent and selective BRD9 and BRD7 inhibitor; orally active

Chemical Name:

4-[4-[(Dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-1,2-dihydro-2,7-naphthyridin-1-one

Purity:

≥98%

(-)-JQ1

Catalog #: 5603

Citations (74)

Product Documents

Images (1)

Negative control for (+)-JQ1

Chemical Name:

(6R)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid 1,1-dimethylethyl ester

Purity:

≥98%

LP 99

Catalog #: 5496

Product Documents

Images (1)

Selective BRD7 and BRD9 inhibitor

Chemical Name:

N-[(2R,3S)-2-(4-Chlorophenyl)-1-(1,2-dihydro-1,4-dimethyl-2-oxo-7-quinolinyl)-6-oxo-3-piperidinyl]-2-methyl-1-propanesulfonamide

Purity:

≥98%

ent-LP 99

Catalog #: 5497

Product Documents

Images (1)

Negative Control for LP 99

Chemical Name:

N-[(2S,3R)-2-(4-Chlorophenyl)-1-(1,2-dihydro-1,4-dimethyl-2-oxo-7-quinolinyl)-6-oxo-3-piperidinyl]-2-methyl-1-propanesulfonamide

Purity:

≥98%

NVS-CECR2-1

Catalog #: 5744

Citations (2)

Product Documents

Images (1)

Potent and selective CECR2 inhibitor

Chemical Name:

N-Cyclopropyl-2-(propylsulfonyl)-6-(1-(2,2,6,6-tetramethylpiperidin-4-yl)-1H-indol-5-yl)pyrimidin-4-amine

Purity:

≥98%

BAY 299

Catalog #: 5970

Citations (2)

Product Documents

Images (1)

Potent and selective BRD1 and TAF1 inhibitor

Chemical Name:

6-(3-Hydroxypropyl)-2-(1,3,6-trimethyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl)-1H-benzo[de]isoquinoline-1,3(2H)-dione

Purity:

≥98%

TP 472N

Catalog #: 5999

Citations (1)

Product Documents

Images (1)

Negative control for TP 472

Chemical Name:

1-(8-(2-(Cyclopropylmethoxy)phenyl)pyrrolo[1,2-a]pyrimidin-6-yl)ethanone

Purity:

≥98%

TP 472N

Catalog #: 5999

Citations (1)

Product Documents

Images (1)

Negative control for TP 472

Chemical Name:

1-(8-(2-(Cyclopropylmethoxy)phenyl)pyrrolo[1,2-a]pyrimidin-6-yl)ethanone

Purity:

≥98%

Bromodomain Inhibitors Small Molecules and Peptides

(+)-JQ1

MZ 1

I-BET 151 dihydrochloride

dBRD9

XMD 8-92

I-BRD9

cis MZ 1

dBET1

dBRD9-A

dBET6

PFI 1

Bromosporine

SGC-CBP30

PFI 3

BAZ2-ICR

CPI 203

NI 57

BI 9564

(-)-JQ1

LP 99

ent-LP 99

NVS-CECR2-1

BAY 299

TP 472N

TP 472N

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