Epigenetic Reader Domain

VTP50469 is a highly selective and orally active inhibitor of Menin-MLL interaction( Ki: 104 pM) and has potently anti-leukemia activity.

Glycodeoxycholic Acid is an endogenous metabolite, a natural product found in Streptomyces niger, Trypanosoma brucei, and Cryptomonas, which induces hepatocyte necrosis and autophagy in patients with obstructive cholestasis.

Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.

SNDX-5613 is a potent and specific inhibitor of Menin-MLL(Ki of 0.149 nM and a cell based IC50 of 10-20 nM). SNDX-5613 can be used for the research of MLL-rearranged (MLL-r) acute leukemias.

(+)-JQ-1 (JQ1) is a BET bromine domain inhibitor that inhibits BRD4 (1 2) (IC50=77 33 nM) with specificity and reversibility. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

666-15 (CREB inhibitor) is a potent and selective CREB inhibitor (IC50: 81 nM).

Naphthol AS-E (nAS-E) is an the KIX-KID interaction and CREB-mediated gene transcription inhibitor.

UNC926 hydrochloride is a methyl-lysine (Kme) reader domain inhibitor.

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.

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.

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

NEO2734 (EP31670) is an orally active and selective inhibitor of p300/CBP and BET bromodomain(IC50 of <30 nM for both p300/CBP and BET bromodomains).

ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS.

BRM/BRG1 ATP Inhibitor-1 is an allosteric dual Brahma homolog (BRM)/SWI/SNF related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and BRG1/SMARCA4 ATPase activity inhibitor (IC50s<0.005 μM).

A-366 is a highly selective peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP, respectively.It is more than 1,000-fold selective for G9a and GLP over the other 21 methyltransferases. It is an inhibitor of the Spindlin1-H3K4me3 interaction with an IC50 of 182.6 nM.It exhibits high affinity for human H3R with a Ki value of 17 nM, and shows subtype selectivity between subgroups of the histaminergic and dopaminergic receptor families.

SGC-CBP30 is an effective CREBBP/EP300 inhibitor (IC50: 21/38 nM).

I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP p300 bromodomains.

dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.

I-BET151 (GSK1210151A) (GSK1210151A) is a specific BET inhibitor for BRD2/3/4 (IC50: 0.5/0.25/0.79 μM, in cell-free assays).

C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay).

CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor.

Menin-MLL inhibitor MI-2 (MI2) is a potent menin-MLL interaction inhibitor with IC50 of 446 nM.

KG-501 (Naphthol AS-E phosphate) is a cAMP response element-binding protein (CREB) inhibitor(IC50 : 6.89 μM).

JQ-1 (carboxylic acid) is a cell-permeable BRD4 inhibitor with IC50s of 77 nM for BRD4(1) and 33 nM for BRD4(2)

BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.

Birabresib (MK-8628) is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity.

BI-7273 is an effective, specific, BRD9 BD Inhibitor, which can infiltrate cell.

dCBP-1 is a chemical degrader of p300 CBP. dCBP-1 hijacks the E3 ubiquitin ligase CRBN for selective degradation of p300 CBP. Degradation of p300 CBP by dCBP-1 leads to effective multiple myeloma cell killing.

Anacardic Acid (6-pentadecylsalicylic Acid) is an effective inhibitor of p300 and p300 CBP-associated factor histone acetyltranferases. It also has antimicrobial activity, antibacterial activity, and inhibits prostaglandin synthase, lipoxygenase, and tyrosinase.

I-BRD9 (GSK602) is the first selective cellular inhibitor for BRD9 with pIC50 of 7.3.

GSK8573 is an inactive control compound for GSK2801. GSK8573 has binding activity to BRD9 (Kd of 1.04 μM).

ODM-207 (BET-IN-4) is a potent BRD4 inhibitor.

MS402 is a novel BD1-selective BET BrD inhibitor.

I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors. I-CBP112 (1 mM) has little activity against other bromodomains. I-CBP112 targets the CBP p300 bromodomains. I-CBP112 significantly reduced the leukemia-initiating poten

BRD4 Inhibitor-10 is an inhibitor of BRD4-BD1 (IC50: 8 nM).

RVX-297 is a BD2 selective inhibitor of BET bromodomains. RVX-297 preferentially binds to the BD2 domains of the BET bromodomain and Extra Terminal (BET) family of protein.

BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.

FL-411 (BRD4-IN-1) is a potent and selective BRD4 inhibitor with an IC50 of 0.43±0.09 μM for BRD4.

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

BRD4 Inhibitor-24 is a BRD4 small molecule inhibitor with antitumor activity.

UNC926 (UNC-926) inhibits L3MBTL1 (IC50: 3.9 μM). UNC926 also exhibits a low micromolar affinity for L3MBTL3. UNC926 inhibits binding of the 3xMBT domain to H4K20me1. It selectively and dose-dependently inhibits the L3MBTL13xMBT-H4K20me1 interaction. UNC926 has not an effect on the binding of 53BP1 to H4K20me1.

GNE-781 is a highly potent and selective inhibitor of CBP (IC50: 0.94 nM in TR-FRET assay). GNE-781 also inhibits BRET and BRD4(1) (IC50s: 6.2 nM and 5100 nM, respectively).

PF-CBP1 hydrochloride (PF-CBP1 HCl) is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.

MI-2-2 is an inhibitor of bivalent protein-protein interaction between menin and MLL with an IC50 of 46 nM. MI-2-2 binds to menin with Kd of 22 nM.

PFI-3 is a selective chemical inhibitor for SMARCA (2/4) (Kd = 89 nM)and PBI (5) bromodomains which may result in the delay and prevention of breast cancer.

EML 425 is a potent and selective inhibitor of CREB binding protein (CBP)/p300 (IC50s: 2.9 and 1.1 μM, respectively).

GSK-5959 is an effective, specific and cell permeable BRPF1 bromodomain inhibitor (IC50: ~80 nM). The selectivity of GSK-5959 for BRPF1 is >100-fold over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.

UMB298 is a potent and selective CBP/P300 bromodomain inhibitor. UMB298 inhibits BRD4 with IC50 of 5193nM.

INCB057643 is a potent, selective and orally bioavailable BET inhibitor.

OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain.