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T6859 |
I-BRD9
|
GSK602 |
Epigenetic Reader Domain
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|
I-BRD9 (GSK602) is the first selective cellular inhibitor for BRD9 with pIC50 of 7.3. |
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T9552 |
BAZ1A-IN-1
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|
Epigenetic Reader Domain
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BAZ1A-IN-1 is a potent BAZ1A inhibitor with the KD value of 0.52 μM for the BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-survival activity against cancer cell lines with high BAZ1A expression, but weak or no activity ag... |
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T8609 |
6-Bromo-3-methyl-1,4-dihydroquinazolin-2-one
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|
Epigenetic Reader Domain
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CHEMBRDG-BB 7118966 is an inhibitor of Bromodomain-containing protein 4 (human). |
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T6032 |
Birabresib
|
OTX-015,OTX015 （MK 8628/Birabresib）,MK-8628 |
Epigenetic Reader Domain
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|
Birabresib (MK-8628) is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity. |
|
T8601 |
1-benzyl-2-ethyl-4,5,6,7-tetrahydro-1H-indol-4-one
|
4H-Indol-4-one, 2-ethyl-1,5,6,7-tetrahydro-1-(phenylmethyl)- |
Epigenetic Reader Domain
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|
1-benzyl-2-ethyl-4,5,6,7-tetrahydro-1H-indol-4-one is an inhibitor Bromodomain-containing protein 4 (human). |
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T6222 |
PFI-1
|
PF-6405761,PFI 1,PFI1 |
Apoptosis
,
Epigenetic Reader Domain
,
Autophagy
|
|
PFI-1 (PF-6405761), a specific BET (bromodomain-containing protein) inhibitor for BRD4, is with the IC50 of 0.22 μM in a cell-free assay. |
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T31221 |
DBRD9
|
dBRD-9,dBRD 9 |
PROTACs
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|
dBRD9 is a PROTAC. dBRD9 is a double-acting molecule, partially containing Bromodomain-containing protein 9 (BRD9), ligand that recruits the cereblon E3 ubiquitin ligase. Ligand that recruits the cereblon E3 ubiquitin li... |
|
T3712 |
Mivebresib
|
ABBV-075 |
Apoptosis
,
Epigenetic Reader Domain
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|
Mivebresib (ABBV-075), also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing protein) with potential antineoplastic activity. Upon administration, the bromodomain inhibitor ABBV-075 binds to the... |
|
TQ0083 |
NI-57
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|
Epigenetic Reader Domain
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|
NI-57 is an inhibitor of proteins of bromodomain and plant homeodomain finger-containing (BRPF) family, with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively. |
|
T6828 |
ZL0420
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|
Epigenetic Reader Domain
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|
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... |
|
T4247 |
I-CBP112 hydrochloride
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|
Epigenetic Reader Domain
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I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors. I-CBP112 (1 mM) has little activity against other bromodomains. I-CBP112 targets the CBP/p300 bromodomains. I-CBP112 significantly re... |
|
T10526 |
β-NF-JQ1
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|
Others
,
PROTACs
|
|
β-NF-JQ1 is a PROTAC that recruits aryl hydrocarbon receptor E3 (AhR E3) ligase to target proteins. β-NF-JQ1 uses β-NF as an AhR ligand to target bromodomain (BRD)-containing proteins and induce AhR and BRD protein inter... |
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T10773 |
CF53
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|
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... |
|
T15627 |
(S)-JQ-35
|
TEN-010 |
Others
|
|
(S)-JQ-35 (TEN-010) is an inhibitor of the Bromodomain and Extra-Terminal (BET) family bromodomain-containing proteins. It has a potential antineoplastic activity. |
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T17294 |
ZL0454
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|
Epigenetic Reader Domain
|
|
ZL0454 is an effective and selective Bromodomain-containing protein 4 inhibitors (IC50: 49 and 32 nM for BD1 and BD2). |
|
T12113 |
MS645
|
|
Epigenetic Reader Domain
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|
|
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T28630 |
RX-37
|
RX37 |
|
|
RX-37 is a potent BET inhibitor with Ki values of 3.2-24.7 nM for BRD2, BRD3 and BRD4. RX-37 demonstrates high selectivity over other non-BET bromodomain-containing proteins. RX-37 potently and selectively inhibits cell ... |
|
T81383 |
PROTAC BRD9 Degrader-5
|
|
PROTACs
|
|
PROTAC BRD9 Degrader-5 is a proteolysis targeting chimera (PROTAC) designed for the specific degradation of Bromodomain-containing protein 9 (BRD9). |
|
T77680 |
BRD7-IN-3
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|
Epigenetic Reader Domain
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|
BRD7-IN-3 (compound 1-78) functions as a dual inhibitor targeting the bromodomain-containing proteins BRD7 and BRD9, demonstrating half-maximal inhibitory concentrations (IC50s) of 1.6 μM for BRD7 and 2.7 μM for BRD9, re... |
|
T74919 |
QA-68
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|
|
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QA-68 (QA-68-ZU81), a potent bromodomain-containing protein 9 (BRD9) degrader, effectively inhibits cell cycle progression and cell colony formation. Demonstrating antiproliferative activity, this compound is particularl... |
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T61727 |
HDAC6/8/BRPF1-IN-1
|
|
|
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HDAC6/8/BRPF1-IN-1 is a dual inhibitor that targets HDAC6, HDAC8, and the bromodomain and PHD finger containing protein 1 (BRPF1). It exhibits inhibitory activity against HDAC1, HDAC6, and HDAC8 with IC50 values of 797 n... |
|
T36103 |
TW9
|
TW9 |
|
|
TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 μM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 μ... |
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T21920 |
UMB-32
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|
|
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UMB-32 is a potent and selective BRD4 inhibitor, demonstrating an affinity for BRD4 with a dissociation constant (K d) of 550 nM and an inhibitory concentration 50 (IC 50) of 637 nM. Moreover, UMB-32 exhibits effectivene... |
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T63858 |
I-BET282E
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|
|
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I-BET282E is a pan-inhibitor of eight BET bromodomains and shows selectivity for other representative bromodomain-containing proteins. i-BET282E is able to act on eight BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), BRD4 ... |
|
T78801 |
BRD7-IN-2
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|
Epigenetic Reader Domain
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|
BRD7-IN-2 (compound 2-77) is a potent selective inhibitor of bromodomain-containing protein 7 (BRD7), exhibiting significant anti-proliferative activity in prostate cancer cells. It demonstrates an IC50 of 5.4 μM for BRD... |
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T36800 |
EN219
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|
|
|
EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.1It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50= 470 nM) and inhibits RNF114-induced autoubiquitination and ... |
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T75135 |
FHD-609
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|
|
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FHD-609, an inhibitor and degrader of BRD9 (bromodomain-containing protein 9), targets the ncBAF complex and is useful for researching a broad spectrum of cancers with mutations in a BAF complex subunit. When used alongs... |
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T81675 |
NICE-01
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AP1867-PEG2-JQ1,AP-PEG2-JQ1 |
|
|
NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1) is a bifunctional compound that facilitates the nuclear import of cytosolic cargoes by leveraging the nuclear-localized bromodomain-containing protein 4 (BRD4) as a carrier for thei... |
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T63991 |
BRD4/CK2-IN-1
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|
|
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BRD4/CK2-IN-1 is the first potent, orally active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), acting on both BRD4 (IC50: 180 nM) and CK2 (IC50: 230 nM). In triple-negative breast ... |
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T38381 |
CAY17c
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|
|
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CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and cla... |
