Epigenetic Reader Domain

AU-15330 is a proteolytic targeting chimera (PROTAC) that simultaneously targets SMARCA4, SMARCA2, and PBRM1 for degradation and exhibits cytotoxicity in H3.3K27M cells but not in H3 wild-type cells. [2]

PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

A-485 is a potent and selective catalytic p300 CBP inhibitor with IC50 values of 9.8 nM for p300 and 2.6 nM for CBP.

ICG001 is a β-catenin TCF-mediated transcription inhibitor that selectively blocks β-catenin CBP interaction without interfering with β-catenin p300 interaction. It specifically binds to CREB protein with an IC50 of 3 μM.

(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1 2) with IC50 values of 77 33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

NEO2734 (EP31670) is an orally active, selective inhibitor of p300 CBP and BET bromodomains, with an IC50 of less than 30 nM for both targets.

VTP50469 is a highly selective and orally active small molecule inhibitor of the Menin-MLL protein-protein interaction with potent anti-leukemic activity with a Ki of 104 pM.

Inobrodib (CBP-IN-1) is a potent inhibitor of p300 CBP bromodomain.

Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300 CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.

666-15 is a selective CREB inhibitor with an IC50 of 81 nM. 666-15 can effectively inhibit the growth of breast cancer.

ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4 in all BL cell lines tested.

CPI-0610 carboxylic acid is an effective and selective small molecule inhibitor of bromine domain and outer end (BET) protein as a ligand of PROTAC target protein. CPI-0610 carboxylic acid may have anticancer and anticancer activities.

FHD-286 is an inhibitor of BRM BRG1 ATPase and can be used for studies on the treatment of BAF-related disorders such as acute myeloid leukemia.

Revumenib (SNDX-5613) is a potent and selective oral inhibitor of menin-KMT2A interaction with Ki of 0.149 nM and IC50 between 10 and 20 nM, which can be used in the study of acute leukemia with MLL gene rearrangement.

ICG001 antagonizes Wnt β-catenin TCF-mediated transcription and specifically binds to element-binding protein (CREB)-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.

BI-7273 is an effective, specific, BRD9 BD Inhibitor, which can infiltrate cell.

dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.

AZD5153 6-Hydroxy-2-naphthoic acid (AZD5153) is a potent triazolopyridazine-based Bromodomain (BRD4) and Extraterminal (BET) inhibitor utilized in cancer treatments.

BBC0403 is a selective BRD2 inhibitor that inhibits BRD2 and BRD2, suppressing NF-κB and MAPK signaling pathways. It can be used in osteoarthritis (OA) research.

Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP p300 family with potential antitumour activity and is palatable for cancer research.

A947 is a potent and selective SMARCA2 protein hydrolysis-targeted chimeric molecule (PROTAC) that induces the degradation of SMARCA2 by binding to VHL E3 ubiquitin ligase, with significant antitumor activity in vivo and in vitro, especially in SMARCA4-mutant non-small cell lung cancer (NSCLC) cells.

GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).

ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2 3 4. It is used in the research on inflammatory diseases, cancer, and AIDS.

C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay).