epigeneticreaderdomain

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.

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.

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.

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]

NSC 228155 is an activator of EGFR, binding to the sEGFR dimerization domain II and modulating EGFR tyrosine phosphorylation.

BY27, a potent and selective BET BD2 inhibitor (Ki: 3.1 nM) with anticancer activity, inhibits BD1/BD2 of BRD2, BRD3, BRD4, and BRDT, and suppresses tumor growth.

AW68 is a potential small molecule BRD4 inhibitor that prevents and treats BRD4-related diseases and can be used in cancer research.

CF53 is a highly potent, selective, and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM, and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, being very selective over non-BET bromodomain-containing proteins. CF53 exhibits potent anti-tumor activity both in vitro and in vivo.

FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional compound that selectively degrades the BET bromodomain transcriptional co-activator BRD4 by linking BET bromodomains to the E3 ubiquitin ligase CRBN. It also functions as a degrader of FKBP12F36V when FKBP12F36V is expressed in-frame with a targeted protein.

LT052 is a selective and efficient BET BD1 inhibitor with anti-inflammatory activity. It mediates the BRD4/NF-κB/NLRP3 inflammatory signaling pathway and can be used in gout arthritis research.

OXFBD04 is a potent and selective BRD4 inhibitor (IC50= 166 nM), a BET bromodomain ligand with modest affinity for the CREBBP bromodomain, and exhibits anti-cancer activity.

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

Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.

BETd-260, a PROTAC linked by a Cereblon ligand and a BET ligand, has an inhibitory effect on BRD4 protein in leukemic cell lines.

GNE-049 is a highly selective and potent inhibitor designed to target the CREB-binding protein (CBP) with high affinity, exhibiting an IC50 of 1.1 nM for the suppression of BRET and BRD4 activity, which consequently blocks prostate cancer cell proliferation in both in vitro and in vivo models.

CCT077791 is a potent inhibitor of p300 and PCAF histone acetyltransferase activity for cancer research.

Crebinostat is a potent histone deacetylase (HDAC) inhibitor, targeting HDAC1, HDAC2, HDAC3, and HDAC6 with IC50s of 0.7 nM, 1.0 nM, 2.0 nM, and 9.3 nM, respectively. It increases the density of synapsin-1 punctae along dendrites in neurons in vitro, modulates chromatin-mediated neuroplasticity, and enhances memory in mice. Additionally, Crebinostat induces histone H3 and H4 acetylation and enhances the expression of Egr1, a cAMP-responsive element binding protein (CREB) target gene.

GNE-375 is a selective and potent BRD9 inhibitor (IC50: 5 nM).GNE-375 inhibits BRD4, TAF1, and CECR2, and can be used to study epigenetic resistance.

ZEN-3694 (ZEN 3694) is a bromo-structural domain extra-terminal inhibitor (BETi) with activity in androgen signaling inhibitor (ASI) resistance models and can be used in combination with enzalutamide to study metastatic desmoplasia-resistant prostate cancer.

NHWD-870 is an effective and selective inhibitor of BET family bromodomain only binding to BRD2, BRD3, BRD4 (IC50 = 2.7 nM), and BRDT. NHWD-870 exhibits potent anti-tumor efficacies and suppresses cancer cell-macrophage interaction through the increase of tumor apoptosis and inhibition of tumor proliferation.

CeMMEC1 is an inhibitor of BRD4, and also has a great affinity for TAF1(IC50=0.9 μM).

PBRM1-BD2-IN-7, a selective and cell-active inhibitor targeting the polybromo-1 (PBRM1) bromodomain, demonstrates inhibitory efficacy against PBRM1-BD2 with an IC50 value of 0.29 μM. This compound is utilized in cancer research.

PBRM1-BD2-IN-2, a selective and cell-active inhibitor of the polybromo-1 (PBRM1) bromodomain, exhibits binding affinity and inhibitory activity specifically targeting the PBRM1-BD2 domain, with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. This compound is utilized in cancer research.

PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor with PBRM1-BD2 Kd of 4.4 μM, PBRM1-BD2 IC50 of 0.16 μM, and PBRM1-BD5 Kd of 25 μM; PBRM1-BD2-IN-8 shows anti-cancer activity.