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Home > Inhibitors & Agonists > Epigenetics > Bromodomain

Bromodomain

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Cat. No. Product Name Field of Application Chemical Structure
DC73281 YEATS4 binder 4e Featured
YEATS4 binder 4e stands out as a highly potent and selective small-molecule inhibitor targeting the epigenetic reader YEATS4. It demonstrates a strong binding affinity with a Ki value of 37 nM. Importantly, this compound exhibits remarkable selectivity, showing over 15-fold preference for YEATS4 compared to other members of the YEATS family, including YEATS1, YEATS2, and YEATS3.
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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.
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DC70783 SJ432 Featured
SJ432 (SJ-432) is a potent, highly selective BET BD2 inhibitor with Kd of 6/2 nM (BRD2-BD2/BRD4-BD2), displays 80/152-fold selectivity over BD1, respectively.SJ432 is more water soluble than SJ018 (40 uM vs <0.1 uM).SJ432 potently inhibits MV4-11 cell growth with GI50 of 8 nM, is more effective than JQ1 at reducing levels of MYC protein in NB cell lines, upregulated p21& GADD45H and downregulated CCND2 & ODC1, C-MYC target genes.SJ432 (15 mg/kg, i.p.) significantluy reduced tumor volumes in pediatric NB xenograft SK-N-AS, with essentially no loss in body weight.
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DC8261 (-)-JQ-1 Featured
The (-)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains,it is the negative control of +JQ-1.
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DC73282 ZEN-3694
ZEN-3694 is a novel potent, orally bioavailable BET bromodomain inhibitor, selectively binds to both bromodomains of the BET proteins, inhibiting the interaction of acetylated histone peptide with IC50 values in low nM range.
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DC73280 YEATS4 binder 4d
YEATS4 binder 4d is a potent, selective small-molecule epigenetic reader YEATS4 binder with Ki of 33 nM, >10-fold selectivity over YEATS1, 2 and 3.
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DC73279 XL-126
XL-126 (XL126) is a potent BD1-selective BET inhibitor with SPR binding KD value of 8.9 nM, has 185-fold BD1/BD2 selectivity.
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DC73278 TDI-11055
TDI-11055 (TDI 11055) is a potent, selective and orally bioavailable inhibitor of the acyl-lysine reader ENL/AF9 YEATS domain with IC50 of 0.05 and 0.07 uM, respectively.
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DC73277 SJ1461
SJ1461 (SJ-1461) is a potent and orally bioavailable BET inhibitor with IC50 of 6.8/0.2 nM for BRD4 BD1/BD2, and 1.3/0.1 nM for BRD2 BD1/BD2, respectively.
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DC73276 PFI-6
PFI-6 is a selective small-molecule chemical probe inhibitor for the YEATS domain of MLLT1 and MLLT3 with IC50 of 140 nM and 160 nM, respectively.
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DC73275 IV-275
IV-275 is a next-generation inhibitor of BRG1 and BRM bromodomains, inhibits SWI/SNF complex and enhances DNA damage and cell death in glioblastoma.
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DC73274 IV-255
IV-255 is a next-generation selective inhibitor of BRG1 bromodomain, inhibits SWI/SNF complex and enhances DNA damage and cell death in glioblastoma.
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DC73273 iBRD4-BD1
iBRD4-BD1 is a potent, selective inhibitor of the first BRD4 bromodomain with IC50 of 12 nM, shows 23- to 6200-fold intra-BET selectivity.
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DC73272 HP-4833
HPI-1 is a high affinity BET bromodomain binder with low nM Kd for BRD2/3/4 and about 10-fold lower affinity for BRDT. HPI-1 shows much higher affinity to BD2 of BRD2 (17 nM), than to BD1 (540 nM), no apparent selectivity between BRD2/3/4.
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DC73271 GSK761
GSK761 (GSK-761) is the first small molecule inhibitor of bromodomain-containing protein SP140, inhibits macrophage inflammatory function.
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DC73270 GSK023
GSK023 is a potent, selective BET BD1 domain inhibitor with pIC50 of 7.8 against BRD4 BD1, >100-fold selective over BD2.
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DC73269 GNE-235
GNE-235 (GNE235) is a potent, selective inhibitor of the second bromodomain of polybromo-1 (PBRM1; BAF180; PB1) with KD value of 0.28 uM in BROMOscan assays.
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DC73268 GNE-234
GNE-234 is the negative control compound of the selective PBRM1(2) inhibitor GNE-235.
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DC73267 FHT-2344
FHT-2344 (FHT2344) is a potent, selective inhibitor of SMARCA4 and SMARCA2 (BRG1 and BRM) with IC50 of 26 and 13 nM respectively, the ATPase component of the BAF complex.
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DC73266 EA-89-YM35
BRD9 inhibitor EA-89 is a potent and selective inhibitor that binds to BRD9 in a novel way.
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DC73265 DW-71177
DW-71177 (DW71177) is a potent and BD1-selective BET inhibitor with ITC KD of 6.7 nM (BRD4-BD1), 20-fold selective over BRD4-BD2, exhibits strong antileukemic activity.
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DC73264 DUAL946
DUAL946 is a sub-micromolar inhibitor of both BET and class I & IIb HDAC proteins with IC50 of 0.05/0.25/0.42/14.13/34.89 uM for BRD4/HDAC1/HDAC2/HDAC5/HDAC7/HDAC9, respectively.
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DC73263 Dual PI3K/BET 18DS
Dual PI3K/BET 18DS is a potent, chimeric dual PI3K/BET bromodomain inhibitor, demonstrates high selectivity, nanomolar range cellular potency, and compelling in vivo efficacy.
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DC73262 DDO-8926
DDO-8926 is a potent selective inhibitor of bromodomain and extra-terminal (BET) proteins with Ki values of 15 nM (BRD4 BD1) and 9.5 nM (BRD4 BD2).
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DC73261 CN210
CN210 is a quinazoline-based BET family inhibitor with Kd value of 70 nM for BRD4 (BD1,2) and IC50 of 0.94 uM in MV4-11 viability assay.
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DC73260 CG223
CG223 (CG14223) is a potent and specific inhibitor of BET proteins with Kd of 45 nM for the C-terminal bromodomain of BRD3 (i.e. BRD3(2)) to 370 nM for the N-terminal bromodomain of BRDT (i.e. BRDT(1)).
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DC73259 CG13250
CG13250 (CG 13250, CG250) is a potent, selective and orally bioavailable BET bromodomain inhibitor with Kd of 44 nM (BRD4), IC50 of 1.1 uM (BRD4 BD1+BD2).
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DC73258 CDD-956
CDD-956 is a highly potent, selective BET bromodomain 1 (BET BD1) inhibitor with IC50 of 2.1 and 4.4 nM for BRDT-BD1 and BRD4-BD1 respectively, with high selectivity (>500-fold) over BET BD2 proteins.
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DC73257 CDD-787
CDD-787 is a highly potent, selective BET bromodomain 1 (BET BD1) inhibitor with IC50 of 2.1 and 3.3 nM for BRDT-BD1 and BRD4-BD1, respectively, with high selectivity (>3,000-fold) over BET BD2 proteins.
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DC73256 BI-7190
BI-7190 (BI 7190) is a potent, selective chemical probe targeting the bromodomain of BPTF with binding Kd of 3.5 nM.
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