16 results for "BRD2 Small Molecules and Peptides" in Products
BRD2: Small Molecules and Peptides
BRD2 (bromodomain-containing 2) is a nuclear mitogen-activated kinase that plays a role in transcription of cell-cycle-regulated genes (1). Alternate names for BRD2 include RING3, NAT, RNF3, FSRG1, D6S113E, FLJ31942, DKFZp686N0336, and KIAA9001 (2). BRD2 belongs to the BET (bromodomain/extra terminal domain) family of proteins which contain two tandem bromodomains (BDI and BDII) and an extra-terminal (ET) domain (1, 3). In mammals there are four BET paralogs (BRD2, BRD3, BRD4, and BRDT) which ...
BET bromodomain inhibitor; orally bioavailable
| Alternate Names: | Birabresib |
| Chemical Name: | (6S)-4-(4-Chlorophenyl)-N-(4-hydroxyphenyl)-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 BET bromodomain inhibitor; cell permeable
| 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-acetic acid 1,1-dimethylethyl ester |
| Purity: | ≥98% (HPLC) |
Potent molecular glue Degrader of BET proteins BRD4 and BRD2
| Chemical Name: | tert-Butyl 2-((S)-4-(4-((4'-((S)-6-(2-(tert-butoxy)-2-oxoethyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-[1,1'-biphenyl]-4-carboxamido)methyl)phenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate |
(+)-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) |
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) |
(+)-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) |
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% (HPLC) |
Potent and selective trivalent BET Bromodomain Degrader (PROTAC®)
| Chemical Name: | N,N'-(11-((2-(((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)methyl)-11-methyl-3,6,9,13,16,19-hexaoxahenicosane-1,21-diyl)bis(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)acetamide) |
| Purity: | ≥98% (HPLC) |
Negative control for SIM1 (Cat. No. 7432)
| Chemical Name: | N,N'-(11-((2-(((S)-1-((2S,4S)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)methyl)-11-methyl-3,6,9,13,16,19-hexaoxahenicosane-1,21-diyl)bis(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)acetamide) |
| Purity: | ≥98% (HPLC) |
Potent BET bromodomain PROTAC®; also degrades BRD-tagged chimeric antigen receptors (CAR) in T cells
| Chemical Name: | (2S,4R)-1-((S)-2-(tert-Butyl)-15-((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)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide |
| Purity: | ≥98% (HPLC) |
Potent and selective SMARCA2/4 and PB1(bromo 5)-selective SWI/SNF bromodomain inhibitor
| Chemical Name: | 1,1-Dimethylethyl 4-[3-amino-6-(2-hydroxyphenyl)-4-pyridazinyl]-1-piperazinecarboxylate bromodomains |
| Purity: | ≥98% (HPLC) |
BET bromodomain inhibitor
| Chemical Name: | 2-Methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide |
| Purity: | ≥98% (HPLC) |
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% (HPLC) |
Potent and selective pan-BD2 inhibitor; orally bioavailable
| Alternate Names: | GSK046 |
| Chemical Name: | 4-(Acetylamino)-3-fluoro-N-(trans-4-hydroxycyclohexyl)-5-[(1S)-1-phenylethoxy]benzamide |
| Purity: | ≥98% (HPLC) |
Potent and high affinity BET bromodomain inhibitor; anti-inflammatory; orally bioavailable.
| Alternate Names: | GSK525762A,Molibresib |
| Chemical Name: | (4S)-6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide |
| Purity: | ≥98% (HPLC) |
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% (HPLC) |
