| DC11729 |
GNE-781
Featured
|
GNE-781 is a potent, selective, non-CNS penetrant, orally active CBP/p300 bromodomain inhibitor with IC50 of 0.94/1.2 nM in TR-FRET assays. |
|
| DC5147 |
Molibresib (I-BET-762)
Featured
|
GSK 525762A is a potent small molecule inhibitors that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4). |
|
| DC8360 |
GSK 5959
Featured
|
GSK 5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM). |
|
| DC8766 |
GSK1324726A (I-BET726)
Featured
|
GSK1324726A (I-BET726) is a novel, potent, and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), and BRD4 (IC50= 22 nM). |
|
| DC9831 |
GSK6853
Featured
|
GSK6853 is a potent, soluble, cell active, and highly selective inhibitor of the BRPF1 bromodomain |
|
| DC5183 |
I-BET151
Featured
|
I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM, respectively. |
|
| DC9658 |
I-BRD9
Featured
|
I-BRD9 is a potent and selective BRD9 inhibitor (pIC50 = 7.3). Exhibits >70-fold selectivity for BRD9 over a panel of 34 other bromodomains and >700-fold selectivity over the BET family. |
|
| DC9836 |
Mivebresib(ABBV-075）
Featured
|
Mivebresib is a novel BET family inhibitor, disrupts critical transcription programs that drive prostate cancer growth to induce potent anti-tumor activity in vitro and in vivo. |
|
| DC7682 |
MS417
Featured
|
MS417 is a novel BrD inhibitor with high affinity and specificity For the BrDs of BET proteins. pIC50 7.52 (IC50 30 nM). |
|
| DC11063 |
MS645 |
MS645 (MS-645) is a novel, bivalent bromodomain (BRD) inhibitor with Ki of 18.4 nM for tandem BD1-BD2 (BRD4 BD1/BD2 ), shows12- to 28-fold gain in affinity for binding to the tandem BD1-BD2 over the single BD1 or BD2. |
|
| DC10023 |
MT-1
Featured
|
MT1 is a bivalent chemical probe of BET bromodomains.MT1 is an intramolecular bivalent BRD4 binder that is more than 100-fold more potent, in cellular assays, than the corresponding monovalent antagonist, JQ1. |
|
| DC9758 |
NI-57
Featured
|
NI-57 is a potent inhibitor of the bromodomains of BRPF proteins that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively, as determined by isothermal titration calorimetry. |
|
| DC7850 |
OF-1
Featured
|
OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with Kd of 100 nM and 500 nM, respectively. |
|
| DC9305 |
PF-CBP1(PF-06670910) hydrochloride
Featured
|
PF-CBP1 is potent and highly-selective inhibitor of the bromodomain of CREB binding protein (CBP BRD) that down regulates targets of CBP in macrophages primary neurons. |
|
| DC5025 |
PFI-1 (PF-6405761)
Featured
|
PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM. |
|
| DC7649 |
PFI-3
Featured
|
PFI-3 is a novel potent, selective and cell permeable inhibitor of SMARCA4 and PB1(5) bromodomains with IC50 ~ 89 nM and 48 nM respectively. |
|
| DC8291 |
PFI-4
Featured
|
PFI-4 is a potent and selective BRPF1 bromodomain inhibitor (IC50 = 80 nM). |
|
| DC10786 |
PLX51107
Featured
|
PLX51107 is a novel BET inhibitor with a unique binding mode in the acetylated lysine binding pocket of BRD4 that differentiates it from other compounds under investigation. |
|
| DC12248 |
PROTAC BET degrader-2 |
PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression. |
|
| DC11041 |
QCA276 |
QCA276 is a novel potent BET proteins inhibitor with IC50/Ki of 10/.3 nM, QCA276 is the BET ligand for PROTAC QCA570. |
|
| DC8320 |
RVX-208
Featured
|
RVX-208(RVX 000222) is a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo; is a BET bromodomain antagonist. |
|
| DC8261 |
(-)-JQ-1
Featured
|
The (-)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains，it is the negative control of +JQ-1. |
|
| DC10190 |
TPOP146 |
TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4. |
|
| DC10066 |
XD14
Featured
|
XD14 is a BET bromodomain inhibitor with Kd values of 160, 170, 380, 490, 830 and 850 nM for BRD4(1), BRD2(1), BRD3(1), BRD3(2), BRD2(2) and BRD4(2) respectively. |
|
| DC11261 |
ZL0420
Featured
|
ZL0420 is a potent, highly selective BRD4 inhibitor with IC50 of 27 and 32 nM for BRD4-BD1 and BRD4-BD2, respectively. |
|
| DC31037 |
IBET151-Az |
IBET151-Az is a IBET151 derivative for PROTAC synthesis.. |
|
| DC31039 |
JQ1-Az |
JQ1-Az is a JQ1 derivative.. |
|
| DC31040 |
FT-1101 |
FT-1101 is a potent pan-BET bromodomain inhibitor that displays equipotent inhibition for BRD2, BRD3, BRD4, and BRDT with Kd < 20 nM. |
|
| DC31043 |
PF-CBP1 hydrochloride |
A potent, highly selective inhibitor of the CBP and p300 bromodomains with IC50 of 125 nM and 363 nM, respectively. |
|
| DC31053 |
GSK525768A |
GSK525768A is an enantiomer, negative control compound of I-BET762 (GSK525762A), shows no activity against BET family proteins BRD2, BRD3 and BRD4.. |
|
