epigenetic

Tazemetostat (EPZ6438) is a histone methyltransferase EZH2 inhibitor (IC50=11 nM) that is orally active, selective, and SAM-competitive. Tazemetostat exhibits antitumor activity and may be used for the treatment of epithelioid sarcoma/follicular lymphoma.

Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM).

L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium) is an epigenetic modifier and putative oncometabolite in renal cancer. L-2-Hydroxyglutaric acid inhibits mitochondrial creatine kinase (Mi-CK) activity(Km and Ki of 2.52 mM and 11.13 mM, respectively).

MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 of 34 nM and 43 nM, respectively.

Epigenetic Multiple Ligand is a cell-permeable inhibitor of substrate processing by several chromatin-associated enzymes, including SIRT1 2, H3 SET7, H3 p300 CBP, H4 RmtA, PABP1 CARM1, and H4 PRMT1. It acts by inducing either apoptosis or granulocytic differentiation.

Epigenetic factor-IN-1 (40569Z) is an inhibitor that exhibits potent binding affinity for SIRT7 and is utilized in the study of liver cancer [1].

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

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]

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.

D18 is an immune modulator that acts as a dual agonist for TLR7 8 (with EC50 values of 24 nM for hTLR7 and 10 nM for hTLR8, respectively). It enhances the expression of PD-L1 through epigenetic regulation, thereby increasing the sensitivity of tumors to PD-1 PD-L1 blockade. Additionally, D18 functions as a cytotoxin for ADC synthesis, specifically for the ADC HE-S2 [1].

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.

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.

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.

GSK-3484862 is a non-covalent Dnmt1 inhibitor that induces DNA hypomethylation, offering potential therapeutic benefits against cancer.

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.

PNZ5, an isoxazole-based pan-BET inhibitor, demonstrates potent activity and high selectivity comparable to the established (+)-JQ1, exhibiting a dissociation constant (KD) of 5.43 nM for BRD4(1).

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