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Search Results for " bd2 "

Targets

77

Compounds

6

Recombinant Proteins

Cat No. Product Name Synonyms Targets
T60155 PBRM1-BD2-IN-7 Epigenetic Reader Domain
PBRM1-BD2-IN-7, a selective and cell-active inhibitor targeting the polybromo-1 (PBRM1) bromodomain, demonstrates inhibitory efficacy against PBRM1-BD2 with an IC50 value of 0.29 μM. This compound is utilized in cancer r...
T60159 PBRM1-BD2-IN-5 Epigenetic Reader Domain
PBRM1-BD2-IN-5 is a potent inhibitor of the PBRM1 Bromodomain, demonstrating dissociation constant (Kd) values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and boasts an inhibitory concentration 50 (IC...
T60156 PBRM1-BD2-IN-2 Epigenetic Reader Domain
PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 ...
T60157 PBRM1-BD2-IN-8 Epigenetic Reader Domain
PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor (PBRM1-BD2 Kd=4.4 μM, PBRM1-BD2 IC50=0.16 μM; PBRM1-BD5 Kd=25 μM). PBRM1-BD2-IN-8 shows anti-cancer activity.
T60158 PBRM1-BD2-IN-3 Epigenetic Reader Domain
PBRM1-BD2-IN-3 (compound 12) is a potent inhibitor of PBRM1-BD2, exhibiting an IC50 value of 1.1 μM, and is utilized in anticancer research.
T8932 GSK046 iBET-BD2 Epigenetic Reader Domain
GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins(IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively). It has immunom...
T72841 PBRM1-BD2-IN-1
PBRM1-BD2-IN-1 is a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, displaying binding affinity and inhibitory efficacy with Kd and IC50 values of 0.7 μM and 0.2 μM, respectively. This compoun...
T72843 PBRM1-BD2-IN-6
PBRM1-BD2-IN-6, a potent inhibitor of the PBRM1 bromodomain, exhibits an IC50 value of 0.22 µM and demonstrates antiproliferative activity. It holds potential for research in PBRM1-dependent cancer treatment.
T79527 BET BD2-IN-1 Epigenetic Reader Domain
BET BD2-IN-1 (compound 45) is a potent, selective inhibitor of BET BD2, exhibiting an IC50 value of 1.6 nM. It suppresses Th17 cell differentiation through the reduced activation of STAT3 and NF-κB, making it relevant in...
T79542 SGC-UBD253 HDAC
SGC-UBD253 is a potent antagonist of the HDAC6-UBD interaction and may be utilized in cancer research [1].
T22345 INCB054329 INCB-054329,INCB-54329,INCB-54329 Epigenetic Reader Domain
INCB054329, a structurally distinct bromodomain and extraterminal domain (BET) inhibitor, inhibits BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2 with IC50 values of 44 nM, 5 nM, 9 nM, ...
T28628 RVX-297 RVX297 Epigenetic Reader Domain
RVX-297 is a BD2 selective inhibitor of BET bromodomains. RVX-297 preferentially binds to the BD2 domains of the BET bromodomain and Extra Terminal (BET) family of protein.
T13392 ZEN-3219 Others , Epigenetic Reader Domain
ZEN-3219 is a BET inhibitor, which has inhibitory effect on BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2). ZEN-3219 has inhibitory effect on BRD4(BD1), The IC50 values of BRD4(BD2) and BRD4(BD1BD2) were 0.48, 0.16 and 0.47 μM, r...
T12112 MS402 Epigenetic Reader Domain
MS402 is a novel BD1-selective BET BrD inhibitor.
T70375 ZEN-2759 Epigenetic Reader Domain
ZEN-2759 is a potent BET small molecule inhibitor of BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2).
T13393 ZEN-3411 Epigenetic Reader Domain
ZEN-3411 is an orally available and potent BET inhibitor that inhibits BRD4(BD1), BRD4(BD2), and BRD4(BD1BD2) and suppresses the growth of tumor cells overproducing BET proteins.
T13394 ZEN-3862 ZEN3862,ZEN 3862 Epigenetic Reader Domain
ZEN-3862 (Willardiine) is an inhibitor of BET(IC50s of 0.16 and 0.13 μM for BRD4(BD1) and BRD4(BD2) , respectively). ZEN-3862 can be used to form PROTACs to induce degradation of BRD4.
T78555 BRD4 Inhibitor-27 Epigenetic Reader Domain
BRD4 Inhibitor-27 is a potent BRD4 inhibitor that inhibits BRD4 BD1 and BRD4 BD2 with IC50s of 9.6 and 11.3 μM, respectively.BRD4 Inhibitor-27 has anticancer activity and can be used for breast cancer research.
T64117 BRD4-BD1-IN-2 Epigenetic Reader Domain
BRD4-BD1-IN-2 is a selective and potent BRD4-BD1 inhibitor with an IC50 value of 2.51 µM, which is 20-fold greater than the inhibitory activity against BRD4-BD2.BRD4-BD1-IN-2 can be used in the study of cardiovascular an...
T16154 MS417 GTPL7512 Epigenetic Reader Domain , HIV Protease
MS417 (GTPL7512) is an inhibitor of BET-specific BRD4(BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively), with weak selectivity at CBP BRD with IC50 of 32.7 μM.
T9020 GSK620 Epigenetic Reader Domain
GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics.GSK620 is highly selective for the BET-BD...
T6828 ZL0420 Epigenetic Reader Domain
ZL0420 is a potent and selective bromodomain-containing protein 4 ( BRD4 ) inhibitor with nanomolar binding affinities to bromodomains (BDs) of BRD4. ZL0420 has IC 50 values of 27 nM against BRD4 BD1 and 32 nM against B...
T9619 I-BET567
I-BET567, a potent pan-BET inhibitor with oral activity, demonstrates pIC50 values of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. This compound has exhibited efficacy in mouse models of oncology and inflammation [1].
T10773 CF53 Epigenetic Reader Domain , CDK
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT B...
TQ0253 PLX51107 Epigenetic Reader Domain
PLX51107 is a potent and selective BET inhibitor (Kds: 1.6, 2.1, 1.7, and 5 nM for BRD2-BD1, BRD3-BD1, BRD4-BD1, and BRDT-BD1).
T5434 ARV-825 Epigenetic Reader Domain
ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4 in all BL cell lines tested.
T2480 Apabetalone RVX-208,RVX000222 Epigenetic Reader Domain , HIV Protease
Apabetalone (RVX000222) , an effective BET bromodomain inhibitor, has been investigated for the treatment of diabetes, atherosclerosis, and coronary artery disease.
T4697 ABBV-744 ABBV744 Epigenetic Reader Domain , HIV Protease
ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS.
T10638 BY27 Epigenetic Reader Domain
BY27 is a potent and selective BET BD2 inhibitor (Ki: 3.1 nM) with anticancer activity, inhibits BD1/BD2 of BRD2, BRD3, BRD4 and BRDT, and suppresses tumor growth.
T17294 ZL0454 Epigenetic Reader Domain
ZL0454 is an effective and selective Bromodomain-containing protein 4 inhibitors (IC50: 49 and 32 nM for BD1 and BD2).
T15484 HJB97 Epigenetic Reader Domain
HJB97 is used for the design of potential PROTAC BET degrader. It also has antitumor activity. HJB97 is a high-affinity inhibitor of BET (Kis: 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2...
T78682 SJ1461 Epigenetic Reader Domain
SJ1461 is a potent, orally active inhibitor of the BET family, selectively targeting and inhibiting BRD2 (BD1), BRD2 (BD2), BRD4 (BD1), and BRD4 (BD2) with respective IC50 values of 1.6 nM, 0.1 nM, 6.5 nM, and 0.2 nM [1]...
T14910 CD161 NKR-P1A Others
CD161 is a potent, selective, and orally bioavailable BET bromodomain inhibitor (IC50s: 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2) with good anticancer activity.
T77590 N1-[5-[[[3-(4-Methoxyphenyl)-1-methyl-1H-indazol-5-yl]carbonyl]amino]-2-methylphenyl]-N4-methyl-1,4-benzenedicarboxamide (ACI)
N1-[5-[[[3-(4-Methoxyphenyl)-1-methyl-1H-indazol-5-yl]carbonyl]amino]-2-methylphenyl]-N4-methyl-1,4-benzenedicarboxamide (ACI) in BD2 DEC-Tec assay with an affinity value of 521 nM.
T77592 N-[5-[[[3-(6-Amino-2-methylpyridin-3-yl)-1-methyl-1H-indazol-5-yl]carbonyl]amino]-2-methylphenyl]-N′-methylterephthalamide
N-[5-[[[3-(6-Amino-2-methylpyridin-3-yl)-1-methyl-1H-indazol-5-yl]carbonyl]amino]-2-methylphenyl]-N′-methylterephthalamide had an IC50 value of 94 nM in a BD2 DEC-Tec assay.
T77591 N-[5-[[[3-(6-Amino-4-methylpyridin-3-yl)-1-methyl-1H-indazol-5-yl]carbonyl]amino]-2-methylphenyl]-N′-methylterephthalamide
N-[5-[[[3-(6-Amino-4-methylpyridin-3-yl)-1-methyl-1H-indazol-5-yl]carbonyl]amino]-2-methylphenyl]-N′-methylterephthalamide had an IC50 value of 22 nM in a BD2 DEC-Tec assay.
T12798 (S)-GNE-987 Epigenetic Reader Domain
(S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC).
T63924 XY153
XY153 (compound 8l) is a BD2 selective BET inhibitor that selectively binds BRD4 BD2. XY153 binds BRD4 BD2 (IC50: 0.79 nM), BRD3 BD2 (IC50: 5.31 nM) and BRD2 BD2 (IC50: 5.09 nM). XY153 can be used to study acute myeloid ...
T63707 BRD4-BD1/2-IN-2
BRD4-BD1/2-IN-2 is a potent inhibitor of BRD4-BD2, capable of acting on both BRD4 BD2 (IC50<0.5 nM) and BRD4 BD1 (IC50<300 nM).
T15419 GS-626510 Epigenetic Reader Domain
GS-626510 is an orally bioavailable inhibitor of BET family bromodomains (Kd: 0.59-3.2 nM for BRD2/3/4; IC50: 83 nM and 78 nM for BD1 and BD2).
T79167 BET-IN-15 Epigenetic Reader Domain
BET-IN-15 (compound 1) is a potent, orally active inhibitor of BET, demonstrating inhibitory IC50 values of 0.64 nM for BRD4-BD1 and 0.25 nM for BRD4-BD2. It exhibits antiproliferative activity [1].
T39601 GSK973 GSK973
GSK973 is a highly selective and orally bioavailable inhibitor that targets the second bromodomains (BD2s) of the BET family. It exhibits a pIC 50 of 7.8 and a pK d of 8.7 specifically for BRD4 BD2. Additionally, GSK973 ...
T39634 GSK097
GSK097 is a highly potent and selective inhibitor of the second bromodomain (BD2) found in bromodomain and extra-terminal domain (BET) proteins. It exhibits a remarkable 2000-fold selectivity for BD2 over BD1, as indicat...
T12113 MS645 Epigenetic Reader Domain
MS645 is an inhibitor of bromodomain-containing protein 4 (BRD4) with a Ki of 18.4 nM for BRD4-BD1/BD2.
T62024 GSK852
GSK852 is a potent, second bromodomain (BD2)-selective, bromo and extra-terminal domain (BET) inhibitor with pIC50 of 7.9.
T40074 PROTAC BRD4 Degrader-15 PROTAC BRD4 Degrader-15
PROTAC BRD4 Degrader-15 is a chemical compound consisting of a PROteolysis TArgeting Chimera (PROTAC) linked to ligands specific to von Hippel-Lindau and BRD4. It exhibits an IC50 of 7.2 nM for BRD4 BD1 and 8.1 nM for BR...
T11441 GNE-987 Epigenetic Reader Domain
GNE-987 is a highly active chimeric BET degrader. GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50: 4.7 and 4.4 nM, respectively). GNE-987 exhibits picomolar cell BRD...
T61318 BRD4 Inhibitor-20 Epigenetic Reader Domain
BRD4 Inhibitor-20 is a potent bromodomain protein 4 (BRD4) inhibitor with oral activity. BRD4 Inhibitor-20 has antiproliferative activity in cancer cell lines and is used in studies of various cancers, such as colon canc...
T74090 PROTAC BRD4 Degrader-7
PROTAC BRD4 Degrader-7, a potent bromodomain BRD4 inhibitor exemplified by compound 1a, demonstrates half-maximal inhibitory concentrations (IC50s) of 15.5 nM and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively [1].
T79018 GSK217 Epigenetic Reader Domain
GSK217 is a potent and selective inhibitor of the bromo and extraterminal domain (BET) second bromodomain (BD2) with high solubility, utilized in oncology and immune inflammation research [1].

Compounds

PBRM1-BD2-IN-7
T60155
Synonym:
Target: Epigenetic Reader Domain
PBRM1-BD2-IN-5
T60159
Synonym:
Target: Epigenetic Reader Domain
PBRM1-BD2-IN-2
T60156
Synonym:
Target: Epigenetic Reader Domain
PBRM1-BD2-IN-8
T60157
Synonym:
Target: Epigenetic Reader Domain
PBRM1-BD2-IN-3
T60158
Synonym:
Target: Epigenetic Reader Domain
GSK046
T8932
Synonym: iBET-BD2
Target: Epigenetic Reader Domain
PBRM1-BD2-IN-1
T72841
Synonym:
Target:
PBRM1-BD2-IN-6
T72843
Synonym:
Target:
BET BD2-IN-1
T79527
Synonym:
Target: Epigenetic Reader Domain
SGC-UBD253
T79542
Synonym:
Target: HDAC
INCB054329
T22345
Synonym: INCB-054329,INCB-54329,INCB-54329
Target: Epigenetic Reader Domain
RVX-297
T28628
Synonym: RVX297
Target: Epigenetic Reader Domain
ZEN-3219
T13392
Synonym:
Target: Others, Epigenetic Reader Domain
MS402
T12112
Synonym:
Target: Epigenetic Reader Domain
ZEN-2759
T70375
Synonym:
Target: Epigenetic Reader Domain
ZEN-3411
T13393
Synonym:
Target: Epigenetic Reader Domain
ZEN-3862
T13394
Synonym: ZEN3862,ZEN 3862
Target: Epigenetic Reader Domain
BRD4 Inhibitor-27
T78555
Synonym:
Target: Epigenetic Reader Domain
BRD4-BD1-IN-2
T64117
Synonym:
Target: Epigenetic Reader Domain
MS417
T16154
Synonym: GTPL7512
Target: Epigenetic Reader Domain, HIV Protease
GSK620
T9020
Synonym:
Target: Epigenetic Reader Domain
ZL0420
T6828
Synonym:
Target: Epigenetic Reader Domain
I-BET567
T9619
Synonym:
Target:
CF53
T10773
Synonym:
Target: Epigenetic Reader Domain, CDK
PLX51107
TQ0253
Synonym:
Target: Epigenetic Reader Domain
ARV-825
T5434
Synonym:
Target: Epigenetic Reader Domain
Apabetalone
T2480
Synonym: RVX-208,RVX000222
Target: Epigenetic Reader Domain, HIV Protease
ABBV-744
T4697
Synonym: ABBV744
Target: Epigenetic Reader Domain, HIV Protease
BY27
T10638
Synonym:
Target: Epigenetic Reader Domain
ZL0454
T17294
Synonym:
Target: Epigenetic Reader Domain
HJB97
T15484
Synonym:
Target: Epigenetic Reader Domain
SJ1461
T78682
Synonym:
Target: Epigenetic Reader Domain
CD161
T14910
Synonym: NKR-P1A
Target: Others
N1-[5-[[[3-(4-Methoxyphenyl)-1-methyl-1H-indazol-5-yl]carbonyl]amino]-2-methylphenyl]-N4-methyl-1,4-benzenedicarboxamide (ACI)
T77590
Synonym:
Target:
N-[5-[[[3-(6-Amino-2-methylpyridin-3-yl)-1-methyl-1H-indazol-5-yl]carbonyl]amino]-2-methylphenyl]-N′-methylterephthalamide
T77592
Synonym:
Target:
N-[5-[[[3-(6-Amino-4-methylpyridin-3-yl)-1-methyl-1H-indazol-5-yl]carbonyl]amino]-2-methylphenyl]-N′-methylterephthalamide
T77591
Synonym:
Target:
(S)-GNE-987
T12798
Synonym:
Target: Epigenetic Reader Domain
XY153
T63924
Synonym:
Target:
BRD4-BD1/2-IN-2
T63707
Synonym:
Target:
GS-626510
T15419
Synonym:
Target: Epigenetic Reader Domain
BET-IN-15
T79167
Synonym:
Target: Epigenetic Reader Domain
GSK973
T39601
Synonym: GSK973
Target:
GSK097
T39634
Synonym:
Target:
MS645
T12113
Synonym:
Target: Epigenetic Reader Domain
GSK852
T62024
Synonym:
Target:
PROTAC BRD4 Degrader-15
T40074
Synonym: PROTAC BRD4 Degrader-15
Target:
GNE-987
T11441
Synonym:
Target: Epigenetic Reader Domain
BRD4 Inhibitor-20
T61318
Synonym:
Target: Epigenetic Reader Domain
PROTAC BRD4 Degrader-7
T74090
Synonym:
Target:
GSK217
T79018
Synonym:
Target: Epigenetic Reader Domain
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Recombinant Proteins

Cat No. Product Name Species Expression System
TMPJ-00667 DEFB4A Protein, Human, Recombinant Human E. coli
β-Defensin 4A is a membrane-active cationic peptide that functions in inflammation and innate immune responses. There are at least 30 β-Defensins, which are distinguished from α-Defensins by the connectivity pattern of t...
TMPH-03361 PLBL2/PLBD2 Protein, Rat, Recombinant (His & SUMO) Rat E. coli
Putative phospholipase. PLBL2/PLBD2 Protein, Rat, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 77.9 kDa and the accession number is Q4QQW8.
TMPH-01677 MBD2 Protein, Human, Recombinant (His & KSI) Human E. coli
Binds CpG islands in promoters where the DNA is methylated at position 5 of cytosine within CpG dinucleotides. Binds hemimethylated DNA as well. Recruits histone deacetylases and DNA methyltransferases. Acts as transcrip...
TMPY-03785 PLBL2/PLBD2 Protein, Human, Recombinant (His) Human HEK293 Cells
PLBL2/PLBD2 Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 62.7 kDa and the accession number is Q8NHP8.
TMPY-06116 PLBL2/PLBD2 Protein, Chinese hamster, Recombinant (His) Chinese hamster CHO Cells
PLBL2/PLBD2 Protein, Chinese hamster, Recombinant (His) is expressed in CHO mammalian cells with His tag. The predicted molecular weight is 63.3 kDa and the accession number is G3I6T1-1.
TMPH-02868 PLBL2/PLBD2 Protein, Mouse, Recombinant (His) Mouse E. coli
Putative phospholipase. PLBL2/PLBD2 Protein, Mouse, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 65.9 kDa and the accession number is Q3TCN2.
TargetMol