IV-255 is a next-generation selective inhibitor of BRG1 bromodomain, inhibits SWI/SNF complex and enhances DNA damage and cell death in glioblastoma.

iBRD4-BD1 is a potent, selective inhibitor of the first BRD4 bromodomain with IC50 of 12 nM, shows 23- to 6200-fold intra-BET selectivity.

HPI-1 is a high affinity BET bromodomain binder with low nM Kd for BRD2/3/4 and about 10-fold lower affinity for BRDT. HPI-1 shows much higher affinity to BD2 of BRD2 (17 nM), than to BD1 (540 nM), no apparent selectivity between BRD2/3/4.

GSK761 (GSK-761) is the first small molecule inhibitor of bromodomain-containing protein SP140, inhibits macrophage inflammatory function.

GSK023 is a potent, selective BET BD1 domain inhibitor with pIC50 of 7.8 against BRD4 BD1, >100-fold selective over BD2.

GNE-235 (GNE235) is a potent, selective inhibitor of the second bromodomain of polybromo-1 (PBRM1; BAF180; PB1) with KD value of 0.28 uM in BROMOscan assays.

GNE-234 is the negative control compound of the selective PBRM1(2) inhibitor GNE-235.

FHT-2344 (FHT2344) is a potent, selective inhibitor of SMARCA4 and SMARCA2 (BRG1 and BRM) with IC50 of 26 and 13 nM respectively, the ATPase component of the BAF complex.

BRD9 inhibitor EA-89 is a potent and selective inhibitor that binds to BRD9 in a novel way.

DW-71177 (DW71177) is a potent and BD1-selective BET inhibitor with ITC KD of 6.7 nM (BRD4-BD1), 20-fold selective over BRD4-BD2, exhibits strong antileukemic activity.

DUAL946 is a sub-micromolar inhibitor of both BET and class I & IIb HDAC proteins with IC50 of 0.05/0.25/0.42/14.13/34.89 uM for BRD4/HDAC1/HDAC2/HDAC5/HDAC7/HDAC9, respectively.

Dual PI3K/BET 18DS is a potent, chimeric dual PI3K/BET bromodomain inhibitor, demonstrates high selectivity, nanomolar range cellular potency, and compelling in vivo efficacy.

DDO-8926 is a potent selective inhibitor of bromodomain and extra-terminal (BET) proteins with Ki values of 15 nM (BRD4 BD1) and 9.5 nM (BRD4 BD2).

CN210 is a quinazoline-based BET family inhibitor with Kd value of 70 nM for BRD4 (BD1,2) and IC50 of 0.94 uM in MV4-11 viability assay.

CG223 (CG14223) is a potent and specific inhibitor of BET proteins with Kd of 45 nM for the C-terminal bromodomain of BRD3 (i.e. BRD3(2)) to 370 nM for the N-terminal bromodomain of BRDT (i.e. BRDT(1)).

CG13250 (CG 13250, CG250) is a potent, selective and orally bioavailable BET bromodomain inhibitor with Kd of 44 nM (BRD4), IC50 of 1.1 uM (BRD4 BD1+BD2).

CDD-956 is a highly potent, selective BET bromodomain 1 (BET BD1) inhibitor with IC50 of 2.1 and 4.4 nM for BRDT-BD1 and BRD4-BD1 respectively, with high selectivity (>500-fold) over BET BD2 proteins.

CDD-787 is a highly potent, selective BET bromodomain 1 (BET BD1) inhibitor with IC50 of 2.1 and 3.3 nM for BRDT-BD1 and BRD4-BD1, respectively, with high selectivity (>3,000-fold) over BET BD2 proteins.

BI-7190 (BI 7190) is a potent, selective chemical probe targeting the bromodomain of BPTF with binding Kd of 3.5 nM.

BI-4827 (BI 4827) is the negative control compound of BI-7190, which is a potent, selective chemical probe targeting the bromodomain of BPTF.

BI 1702135 (Compound 4) is a potent SMARCA2 binder for targeted protein degradation (PROTAC) design as BI 1810284 (ACBI2, Cat. PC-20464).

BBC1115 is a novel chemotype inhibitor of bromodomain and extra-terminal motif (BET) proteins, displays broad binding across BDs of BET proteins.

Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.

SRX3177 is a potent, triple BRD4/PI3K/CDK4/6 inhibitor with nanomolar potency against PI3Kα (IC50=79 nM), BRD4 bromodomains (BD1 and BD2) (IC50=33 nM and 89 nM, respectively), and CDK4/6 (IC50=2.5/3.3 nM).SRX3177 is capable of targeting BRD4, PI3K and CDK4/6 simultaneously, induces apoptosis and cell cycle arrest and has in vitro efficacy in mantle cell lymphoma, hepatocellular carcinoma and neuroblastoma models.SRX3177 has antitumor efficacy in in vivo xenograft models and is less toxic than the combination of agents that inhibit individual targets.

MC2652 (compound 1a) is a potent LSD1 inhibitor. MC2652 displays high inhibiting effects in MV4-11 and NB4 leukaemia cells. MC2652 shows antiproliferative activity against prostate cancer LNCaP cells.

3-deazaneplanocin A (DZNeP), an analog of adenosine, is a competitive inhibitor of S-adenosylhomocysteine hydrolase with Ki of 50 pM.

Ziftomenib is a menin-MLL interaction inhibitor with antitumor activities (WO2017161028A1, compound 151).

AMI-1 is a PRMT and HIV-1 RT polymerase inhibitor.

Bomedemstat (IMG-7289) ditosylate is an oral and irreversible inhibitor of the epigenetically active lysine-specific demethylase 1 (LSD1) in mouse models of myeloproliferative neoplasms (MPNs). Bomedemstat can be used for the research of acute myelogenous leukemia (AML) and myelofibrosis (MF). Antineoplastic activity.

MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC).