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.

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.

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.

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

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.

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.

(+)-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.

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.

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.

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.

5-Ph-IAA, a derivative of Indole-3-acetic acid (IAA), acts as a plant hormone and serves as an enzyme or prodrug combination for cancer gene therapy.

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.

Ziftomenib (KO-539) is an inhibitor of menin-MLL interaction with antitumor activity, suitable for leukemia research.

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.

BRM/BRG1 ATP Inhibitor-1 is an allosteric dual Brahma homolog (BRM)/SWI/SNF related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and BRG1/SMARCA4 ATPase activity inhibitor (IC50s<0.005 μM).

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

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.

I-BET567, a potent pan-BET inhibitor with oral activity, demonstrates pIC50 values of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. This compound has exhibited efficacy in mouse models of oncology and inflammation [1].

YTH-IN-1 is an inhibitor of the five YTH structural domains in the human YTHDF1, YTHDF2, YTHDF3, YTHDC1, and YTHDC2 proteins.The YTH family of proteins is an N 6-methyladenosine (m6A) reader that plays an important regulatory role in gene expression.

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.

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

BRD7-IN-1, a modified derivative of BI7273 (BRD7/9 inhibitor), forms PROTAC VZ185 via linkage to a VHL ligand, demonstrating potent activity against BRD7/9 with DC50 values of 4.5 and 1.8 nM, respectively [1].

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