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.

GSK 525762A is a potent small molecule inhibitors that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4).

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).

Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.

EZM2302 (GSK3359088) is the first potent and selective inhibitor of CARM1 enzymatic activity that exhibits anti-proliferative effects both in vitro and in vivo,in biochemical assays (IC50=6nM) with broad selectivity against histone methyltransferases.

MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM.

GNE-781 is a potent, selective, non-CNS penetrant, orally active CBP/p300 bromodomain inhibitor with IC50 of 0.94/1.2 nM in TR-FRET assays.

EBI-2511 is a highly potent and orally active EZH2 inhibitor for the treatment of Non-Hodgkin’s Lymphoma.

BAY-299 is a potent and selective inhibitor of the bromodomain and PHD finger-containing (BRPF) family protein BRD1 (IC50 = 6 nM).

MDK-7933, also known as HDAC8-IN-1, is a HDAC8 inhibitor with an IC50 of 27.2 nM in cancer cell lines. MDK-7933 shows antiproliferative effects toward several human lung cancer cell lines (A549, H1299, and CL1-5). MDK-7933 was first reported in ChemMedChem. 2012 Oct;7(10):1815-24. MDK-7933 has CAS#1417997-93-3.

SGC-SMARCA-BRDVIII is a potent and selective SMARCA2/4 BRD inhibitor.

Elevenostat (JB3-22) is a selective HDAC11 inhibitor (IC50=0.235 µM). Anti-multiple myeloma (MM) activity.

CTB is a p300 activator and the lowest docked energy for CTB and p300 is 7.72 kcal/mol.

I-BET567 is a potent and oral active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.

JADA82 (PCK82) is a potent KDM5A (lysine demethylase 5A) inhibitor. From patent WO2020033377A1.

A-196 is a potent and selective chemical inhibitor of SUV420H1 and SUV420H2 that inhibits the di- and trimethylation of H4K20me in multiple cell lines.

CeMMEC1 is a novel potent inhibitor of the second bromodomain of TAF1, binding neither the first nor the second bromodomain of BRD4.

ORY-1001 dihydrochloride (RG-6016, Ladademstat) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases.

DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC50 value of 28 nM. DS-9300 has anticancer activity and can be used in prostate cancer disease research.

EZM0414 is a potent, selective, and orally bioavailable inhibitor of Histone-lysine N-methyltransferase SETD2.

SS-208 (SS208) is a novel potent, selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 12 nM, >100-fold selectivity over HDAC1/4/5/7/8/9/11.SS-208 has minimal effects on the viability of murine SM1 melanoma cells in vitro, significantly reduced in vivo tumor growth in a murine SM1 syngeneic melanoma mouse model.

GSK549 (GSK-549) is a potent, highly selective, BD2 domain-selective BET inhibitor with pIC50 of 7.8 (BRD4 BD2), 1150-fold selectivity over BD1.