| DC11503 |
KDOAM-25
Featured
|
A potent, selective KDM5 sub-family(JARID1) inhibitor with biochemical IC50 of 71/19/69/69 nM for KDM5A/B/C/D, respectively. |
|
| DC11724 |
MS-453 |
A potent, selective. covalent protein lysine methyltransferase SETD8 inhibitor with IC50 of 804 nM. |
|
| DC10509 |
A-196
Featured
|
A-196 is a potent and selective chemical inhibitor of SUV420H1 and SUV420H2 that inhibits the di- and trimethylation of H4K20me in multiple cell lines. |
|
| DC7855 |
A-366
Featured
|
A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM). |
|
| DC10129 |
A395
Featured
|
A-395 potently inhibited the formation of H3K27me3 (via antagonizing EED in the trimeric PRC2 complex (EZH2:EED:SUZ12)) with IC50 = 34 ± 2 nM (Hill Slope = 0.7) |
|
| DC11452 |
ABBV-744
Featured
|
ABBV-744 is a BDII-selective BET bromodomain inhibitor that is being investigated to treat AML and metastic castration-resistant prostate cancer.BBV-744, a highly potent and selective inhibitor of the BD2 domain of BET family proteins with drug-like properties. In contrast to the broad range of cell growth inhibition induced by DbBi, the antiproliferative activity of ABBV-744 was largely, but not exclusively, restricted to cell lines of acute myeloid leukaemia and prostate cancer that expressed the full-length androgen receptor (AR). ABBV-744 retained robust activity in prostate cancer xenografts, and showed fewer platelet and gastrointestinal toxicities than the DbBi ABBV-07514.Analyses of RNA expression and chromatin immunoprecipitation followed by sequencing revealed that ABBV-744 displaced BRD4 from AR-containing super-enhancers and inhibited AR-dependent transcription, with less impact on global transcription compared with ABBV-075. These results underscore the potential value of selectively targeting the BD2 domain of BET family proteins for cancer therapy. |
|
| DC8476 |
ACY-738
Featured
|
ACY-738 demonstrates inhibitory activity against recombinant HDAC6 with IC50 values of 1.7 nM, with respective average selectivity over class I HDACs being 100-fold. |
|
| DC11008 |
ACY-957 |
ACY-957 (ACY957) is a potent, selective inhibitor of HDAC1 and HDAC2 with IC50 of 7 and 18 nM, shows limited activity against HDAC3 (IC50=1,300 nM) and no activity against HDAC4/5/6/7/8/9 (IC50>20 nM). |
|
| DC8437 |
AGK2
Featured
|
AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM. |
|
| DC7540 |
SIRT2 Inhibitor II, AK-7
Featured
|
AK-7 is a cell- and brain-permeable inhibitor of SIRT2 (IC50 = 15.5 μM). |
|
| DC11887 |
Alobresib (GS-5829)
Featured
|
Alobresib is a novel BET bromodomain inhibitor with antineoplastic activity.. |
|
| DC8292 |
AMI-1
Featured
|
AMI-1 is a PRMT and HIV-1 RT polymerase inhibitor. |
|
| DC8322 |
Anacardic Acid
Featured
|
Anacardic acid inhibits the histone acetyltransferase (HAT) activity of the transcription co-activators p300 and p300/CREB-binding protein-associated factor (pCAF) with IC50 values of 8.5 and 5 µM, respectively. |
|
| DC10334 |
ARV-771
Featured
|
ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader with Kd values of 4.7, 7.6, 7.6 nM against bromodomain 2, 3 and 4, respectively. |
|
| DC12024 |
ARV-825
Featured
|
ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively. |
|
| DC9840 |
AS-8351
Featured
|
AS 8351 induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes, in combination with CHIR 99021, A83-01, BIX 01294, SC1, Y-27632, OAC2, SU 16f and JNJ 10198409. |
|
| DC8537 |
AZ505
Featured
|
AZ505 is a potent and highly selective inhibitor of the oncogenic protein SMYD2(IC50=0.12 uM) with potential anticancer activity, >600 fold than SMYD3(IC50>83.3 uM); DOT1L(IC50>83.3 uM);EZH2(IC50>83.3 uM). |
|
| DC10288 |
AZD5153 6-Hydroxy-2-naphthoic acid
Featured
|
AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM. |
|
| DC10774 |
AZD5153
Featured
|
AZD5153 is a potent bivalent triazolopyridazine based Bromodomain and Extraterminal (BET) Inhibitor. |
|
| DC12029 |
BAY-299
Featured
|
BAY-299 is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1 (IC50 = 6 nM). |
|
| 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. |
|
| DC7854 |
BAZ2-ICR |
BAZ2-ICR is a selective BAZ2 bromodomain inhibitor (Kd values are 109 and 170 nM for BAZ2A and BAZ2B respectively). |
|
| DC10885 |
BCI-121
Featured
|
BCI-121 is a SMYD3 inhibitor that impairs the proliferation of cancer cell. |
|
| DC7082 |
Belinostat (PXD101)
Featured
|
Belinostat (PXD101) is a novel pan-HDAC inhibitor with IC50 of 27 nM, with activity demonstrated in cisplatin-resistant tumors. |
|
| DC11042 |
BET inhibitor CF53 |
BET inhibitor CF53 is a highly potent, orally active inhibitor of bromodomain and extra-terminal (BET) with Ki of <1 nM (BRD4 BD1). |
|
| DC8556 |
BET-BAY 002 |
BET-BAY 002 is a potent BET inhibitor; shows efficacy in a multiple myeloma model. |
|
| DC8310 |
BG-45
Featured
|
BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM). It inhibits HDAC1, HDAC2, and HDAC6 with greatly reduced potency (IC50s = 2, 2.2, and >20 µM, respectively). |
|
| DC9888 |
BI-9564
Featured
|
BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with Kd of 5.9 nM for BRD9, and IC50 of > 100 μM for BET family. |
|
| DC7374 |
BIX01294
Featured
|
BIX01294 is an inhibitor of G9a histone methyltransferase with IC50 of 2.7 μM. |
|
| DC8660 |
BML-210(CAY10433)
Featured
|
BML-210 is the novel HDAC inhibitor, and its mechanism of action has not been characterized. |
|
