| 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. |
|
| 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. |
|
| 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. |
|
| DC73266 |
EA-89-YM35 |
BRD9 inhibitor EA-89 is a potent and selective inhibitor that binds to BRD9 in a novel way. |
|
| 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. |
|
| DC73268 |
GNE-234 |
GNE-234 is the negative control compound of the selective PBRM1(2) inhibitor GNE-235. |
|
| 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. |
|
| DC73270 |
GSK023 |
GSK023 is a potent, selective BET BD1 domain inhibitor with pIC50 of 7.8 against BRD4 BD1, >100-fold selective over BD2. |
|
| DC73271 |
GSK761 |
GSK761 (GSK-761) is the first small molecule inhibitor of bromodomain-containing protein SP140, inhibits macrophage inflammatory function. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| 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. |
|
| DC73283 |
2,4-lutidine |
2,4-lutidine is a small molecule targeting the UHRF1 tandem Tudor domain (TTD) with TR-FRET (His6-TTD vs. H3K9me3) EC50E of 29.2 uM. |
|
| DC73284 |
F1957-0088 |
F1957-0088 is a small molecule targeting the UHRF1 tandem Tudor domain (TTD) with TR-FRET (TTD vs. H3K9me3) EC50 of 45.1 uM. |
|
| DC73285 |
GSK3482364
Featured
|
GSK-3484862 is a non-covalent inhibitor for DNA methyltransferase (Dnmt1). GSK-3484862 induces DNA hypomethylation to against cancer. GSK-3484862 mediates dramatic demethylation in murine embryonic stem cells with minimal non-specific toxicity. |
|
| DC73287 |
A452 |
A452 is a potent and selective HDAC6 inhibitor, effectively inhibits the cell growth and viability of various cancer cell types, irrespective of p53 status. |
|
| DC73288 |
CM-1758 |
CM-1758 is a novel histone deacetylase (HDAC) inhibitor with IC50 of 5 nM and 126 nM for HDAC1 and HDAC6, respectively. |
|
| DC73289 |
GH8HA01 |
GH8HA01 is a highly potent, selective HDAC8 inhibitor with Ki of 0.67 nM, highly selective against HDAC8 compared to other HDACs. |
|
| DC73290 |
HO53 |
HO53 is a small moecule inducer of cathelicidin antimicrobial peptide gene (CAMP) expression in bronchial epithelium cells, HO53 is a histone deacetylase (HDAC) inhibitor, interacts directly with HDAC3. |
|
| DC73291 |
HR488B |
HR488B is a potent, selective HDAC1 inhibitor with IC50 of 1.24 uM, effectively inhibits the proliferation of CRC cells. |
|
| DC73292 |
KH-259 |
KH-259 is a potent, isozyme-selective and CNS-penetrant HDAC6 inhibitor with IC50 of 260 nM, shows weak activity against HDAC1 and HDAC4 (IC50>6 uM). |
|
| DC73293 |
KPZ560 |
KPZ560 is a potent, HDAC1/2-selective inhibitor with IC50 of 12/68 nM, respectively. |
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