TP-238 is a potent and selective dual CECR2/BPTF probe with pIC50 values of 7.5 and 6.5, respectively. TP-238 also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases.

MT1 is a bivalent chemical probe of BET bromodomains, with an IC50 of 0.789 nM for BRD4(1).

Tucidinostat D4 (Chidamide D4) is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively.

EPZ004777 hydrochloride is a potent, selective DOT1L with IC50 of 0.4 nM.

SETD2-IN-1 TFA is a potent, selective and orally active of SETD2 which is a human histone methyltransferase. SETD2-IN-1 TFA has anti-proliferative effects.

BET-IN-1 is a bromodomain extracted from patent WO/2013024104A1, compound example 2, has a plC50 in the range 6.0 - 7.0.

NHWD-870 is a potent, orally active and selective BET family bromodomain and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation.

(+)-JQ-1-aldehyde is the aldehyde form of (+)-JQ1. (+)-JQ-1-aldehyde can be uesd as a precursor to synthesize PROTACs, which targets BET bromodomains.

A-395 potently inhibited the formation of H3K27me3 (via antagonizing EED in the trimeric PRC2 complex (EZH2:EED:SUZ12)) with IC50 = 34 ± 2 nM (Hill Slope = 0.7)

MPI_5a is a potent selective inhibitor of HDAC6, and poorly blocks other HDAC enzymes.

Tubastatin A TFA (Tubastatin A trifluoroacetate salt) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis.

BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins.

GSK-340 is a potent, selective inhibitor of second bromodomains of the BET family (BD2) with pKd of 8.18, 7.49, 7.72 and 7.68 for BRD4 BD2, BRD3 BD2, BRD2 BD2 and BRD4T BD2, respectively.

GSK4027 (GSK 4027, GSK-4027) is a potent, selective, cell-penetrant chemical probe of PCAF/GCN5 bromodomain with pKi of 8.9 for both.

GSK525768A is an enantiomer, negative control compound of I-BET762 (GSK525762A), shows no activity against BET family proteins BRD2, BRD3 and BRD4..

A potent, highly selective inhibitor of the CBP and p300 bromodomains with IC50 of 125 nM and 363 nM, respectively.

A high-affinity, small-molecule peptidomimetic inhibitor of MLL1/WDR5 protein-protein interaction with Ki of 2.4 nM.

FT-1101 is a potent pan-BET bromodomain inhibitor that displays equipotent inhibition for BRD2, BRD3, BRD4, and BRDT with Kd < 20 nM.

JQ1-Az is a JQ1 derivative..

IBET151-Az is a IBET151 derivative for PROTAC synthesis..

SALL4 peptide FFW (RRKFAKFQWI, FFW peptide) is a potent therapeutic SALL4 peptide antagonist of SALL4-NURD (nucleosome remodeling deacetylase) interaction with target affinity of 23 nM.

MC3482 is a potent, specific SIRT5 inhibitor, increases the ammonia content in cells leading to autophagy and mitophagy, shows selective SIRT5 inhibition vs SIRT1-3.

Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat trihydrochloride inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki of 2.5 nM. Tazemetostat trihydrochloride inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat trihydrochloride inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.

Targaprimir-96 TFA is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 TFA selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 TFA binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 TFA directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells.

Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells.

OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity.

Dot1L-IN-6 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.19 nM.

Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.17 nM.

WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines.

LT052 is a highly selective BET BD1 inhibitor. LT052 displays inhibitory activity against BRD4 (BD1), BRD3 (BD1) and BRDT (BD1) with IC50s of 87.7, 246.3, and 357.1 nM, respectively. LT052 shows nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2. LT052 has inhibitory activities against BRPF1b (IC50=567.5 nM). LT052 has anti-inflammatory activity.