| DC10656 |
(+)-JQ1 carboxylic acid
Featured
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(+)-JQ1 carboxylic acid is the carboxylic acid form of (+)-JQ1 for derivative synthesis. |
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| DC5019 |
(+)-JQ1
Featured
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(+)-JQ1 is a BET bromodomain inhibitor, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. |
-JQ-1.gif)
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| DC12021 |
(+)-JQ1 PA
Featured
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(+)-JQ1 PA is a Click-activated (alkyne) version of the BET bromodomain inhibitor (+)-JQ1. |
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| DC11652 |
Ischemin sodium |
A cell permeable CBP bromodomain inhibitor with Kd of 19 uM. |
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| DC11653 |
Ischemin |
A cell permeable CBP bromodomain inhibitor with Kd of 19 uM. |
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| DC7565 |
BET bromodomain inhibitor,cas 1505453-59-7 |
A new compound which is similar with +JQ-1，BET bromodomain inhibitor |
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| DC11793 |
UMB-32 |
A novel a potent, selective inhibitor of BRD4 with Kd of 550 nM, cellular IC50 of 724 nM. |
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| DC11792 |
UMB-136 |
A novel bromodomain BRD4 inhibitor that significantly induces HIV-1 reactivation. |
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| DC11730 |
GNE-207 |
A novel potent, selective, orally active CBP/p300 bromodomain with IC50 of 1.0 nM. |
|
| DC11568 |
HJB-97 |
A potent BET bromodomian inhibitor with IC50 of 3-7 nM for BRD2/3/4 BD1 and BD2.. |
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| DC11452 |
ABBV-744
Featured
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ABBV-744 is a BDII-selective BET bromodomain inhibitor that is being investigated to treat AML and metastic castration-resistant prostate cancer.BBV-744, a highly potent and selective inhibitor of the BD2 domain of BET family proteins with drug-like properties. In contrast to the broad range of cell growth inhibition induced by DbBi, the antiproliferative activity of ABBV-744 was largely, but not exclusively, restricted to cell lines of acute myeloid leukaemia and prostate cancer that expressed the full-length androgen receptor (AR). ABBV-744 retained robust activity in prostate cancer xenografts, and showed fewer platelet and gastrointestinal toxicities than the DbBi ABBV-07514.Analyses of RNA expression and chromatin immunoprecipitation followed by sequencing revealed that ABBV-744 displaced BRD4 from AR-containing super-enhancers and inhibited AR-dependent transcription, with less impact on global transcription compared with ABBV-075. These results underscore the potential value of selectively targeting the BD2 domain of BET family proteins for cancer therapy. |
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| DC11887 |
Alobresib (GS-5829)
Featured
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Alobresib is a novel BET bromodomain inhibitor with antineoplastic activity.. |
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| DC10334 |
ARV-771
Featured
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ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader with Kd values of 4.7, 7.6, 7.6 nM against bromodomain 2, 3 and 4, respectively. |
|
| DC12024 |
ARV-825
Featured
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ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively. |
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| DC10288 |
AZD5153 6-Hydroxy-2-naphthoic acid
Featured
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AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM. |
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| DC10774 |
AZD5153
Featured
|
AZD5153 is a potent bivalent triazolopyridazine based Bromodomain and Extraterminal (BET) Inhibitor. |
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| DC12029 |
BAY-299
Featured
|
BAY-299 is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1 (IC50 = 6 nM). |
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| DC11505 |
BAY-850
Featured
|
BAY-850 (BAY 850, BAY850) is a potent, isoform selective, cellularly active ATAD2 bromodomain inhibitor with binding IC50 of 166 nM in TR-FRET assay. |
|
| DC7854 |
BAZ2-ICR |
BAZ2-ICR is a selective BAZ2 bromodomain inhibitor (Kd values are 109 and 170 nM for BAZ2A and BAZ2B respectively). |
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| DC11042 |
BET inhibitor CF53 |
BET inhibitor CF53 is a highly potent, orally active inhibitor of bromodomain and extra-terminal (BET) with Ki of <1 nM (BRD4 BD1). |
|
| DC8556 |
BET-BAY 002 |
BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model. |
|
| DC9888 |
BI-9564
Featured
|
BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with Kd of 5.9 nM for BRD9, and IC50 of > 100 μM for BET family. |
|
| DC10609 |
BMS-986158
Featured
|
BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins. |
|
| DC9923 |
CeMMEC1
Featured
|
CeMMEC1 is a novel potent inhibitor of the second bromodomain of TAF1, binding neither the first nor the second bromodomain of BRD4. |
|
| DC5046 |
CPI203 (CPI-203)
Featured
|
CPI203 is a novel potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM (BRD4 α-screen assay). |
|
| DC8619 |
CPI-268456
Featured
|
CPI-268456 is a potential BET bromodomain inhibitor. |
|
| DC10477 |
CPI-637
Featured
|
CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively. |
|
| DC10845 |
FL-411
Featured
|
FL-411 is a selective BRD4 inhibitor. |
|
| DC9934 |
GNE-272 |
GNE-272 is a in Vivo Probe for the Bromodomains of CBP/EP300. |
|
| DC12313 |
GNE-371 |
GNE-371 is a potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like, with an IC50 of 10 nM for TAF1(2). |
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