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Cat No. | Product Name | Synonyms | Targets |
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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]. |
Cat No. | Product Name | Species | Expression System |
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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. |