| DC48411 |
CTB
|
CTB is a p300 activator and the lowest docked energy for CTB and p300 is 7.72 kcal/mol. |
| DC11511 |
A-485
|
A potent, selective and, cell and in vivo active p300/CBP catalytic inhibitor with IC50 of 9.8/2.6 nM. |
| DC73311 |
MC4171
|
MC4171 (KAT8 inhibitor 34) is a first-in-class, selective and reversible lysine acetyltransferase KAT8 inhibitor with IC50 of 8.1 uM and SPR Kd of 2.04 uM. |
| DC73310 |
JG-2016
|
JG-2016 is a small molecule inhibitor of histone acetyltransferase 1 (HAT1) with IC50 of 14.8 uM in the HAT1 acetylation assays. |
| DC71967 |
B026
|
B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines. |
| DC71672 |
EML 425
|
EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC50s of 2.9 and 1.1 μM, respectively. |
| DC71315 |
DS17701585
|
DS17701585 (Compound 11) is a highly selective, orally active EP300 and CBP inhibitor with IC50 values of 0.040, 0.15, 0.45 and 0.70 µM against CBP, EP300, H3K27 and SOX2. DS17701585 can be used for cancer research. |
| DC71021 |
Coumarin-SAHA
|
Coumarin-SAHA is a fluorescent probe for determining the binding affinities (kd) and the dissociation off-rates (koff) of the HDAC8-inhibitor complexes. |
| DC70508 |
IMP-1575
|
IMP-1575 (IMP1575) is a potent, selective Hedgehog acyltransferase (HHAT) inhibitor with Ki/IC50 of 38 nM/0.75 uM (Acyl-cLIP assay).IMP-1575 is the first sub-micromolar small-molecule HHAT inhibitor reported to-date.IMP‐1575 (50-0.023 μM) was therefore analyzed for effects on HHAT kinetics at varying Pal‐CoA concentrations (50–0.19 μM).IMP-1575 is a chemical tool and methodology to provide insight into HHAT which may expedite future studies and drug discovery efforts against this important target class. |
| DC70390 |
ENL YEATS Domain inhibitor 7
|
ENL YEATS Domain inhibitor 7 is a selective, small molecule inhibitor of ENL YEATS Domain with IC50 of 0.62 uM in inhibiting the ENL-acetyl-H3 interaction.ENL YEATS Domain inhibitor 7 displayed strong selectivity toward the ENL YEATS domain over all other human YEATS domains.ENL YEATS Domain inhibitor 7 exhibited on-target inhibition of ENL in cultured cells and a synergistic effect with the bromodomain and extraterminal domain inhibitor JQ1 in killing leukemia cells. |
