Epigenetic Reader Domain Inhibitor

FL-411 (Standard) is the analytical standard of FL-411 (HY-111102). This product is intended for research and analytical applications. FL-411 is a potent and selective BRD4 inhibitor with an IC₅₀ of 0.43±0.09 μM for BRD4(1).

I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (K_ds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin.

SGC-CBP30 (Standard) is the analytical standard of SGC-CBP30 (HY-15826). This product is intended for research and analytical applications. SGC-CBP30, a chemical probe, is a potent and highly selective CBP/p300 bromodomain (K_ds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects.

BRD4 Inhibitor-32 (example 15) is a BRD4 inhibitor that can be used in acute kidney disease and chronic kidney disease research.

ENL/AF9 YEATS-IN-1 is a ENL/AF9 YEATS domain inhibitor. ENL/AF9 YEATS-IN-1 suppresses oncogene expression in cells by inhibiting the ENL/AF9 YEATS domain. ENL/AF9 YEATS-IN-1 can be used in leukemia research.

Revumenib (Standard) is the analytical standard of Revumenib (HY-136175). This product is intended for research and analytical applications. Revumenib (SNDX-5613) is a potent and specific Menin-MLL inhibitor with a binding K_i of 0.149 nM and a cell based IC₅₀ of 10-20 nM. Revumenib can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML).

Y06036 (Standard) is the analytical standard of Y06036 (HY-111502). This product is intended for research and analytical applications. Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with K_d value of 82 nM. Antitumor activity.

Naphthol AS-E (Standard) is the analytical standard of Naphthol AS-E (HY-104068). This product is intended for research and analytical applications. Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (Kd:8.6 μM), blocks the interaction between the KIX domain and the KID domain of CREB with IC₅₀ of 2.26 μM. Naphthol AS-E can be used for cancer research.

MZ 1 (Standard) is the analytical standard of MZ 1 (HY-107425). This product is intended for research and analytical applications. MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. K_ds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively.

666-15 (Standard) is the analytical standard of 666-15 (HY-101120). This product is intended for research and analytical applications. 666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model.

Menin-MLL-IN-36 (compound 398) is an inhibitor of menin/MLL protein/protein interaction with an IC₅₀ value of 0.043 μM in MEIS1 mRNA expression. Menin-MLL-IN-36 can be used in the research of cancer, myelodysplastic syndrome (MDS), myeloproliferative neoplasms (MPN), and diabetes.

Bet-in-24 (example 2) is a bromodomain and extra-terminal (BET) inhibitor. BET-IN-24 can be used in the study of virology, heart failure, inflammation, central nervous system (CNS) diseases and many cancers

E-7386 (Standard) is the analytical standard of E-7386 (HY-111386). This product is intended for research and analytical applications. E-7386 is an orally active CBP/beta-catenin modulator.

BI-7273 (Standard) is the analytical standard of BI-7273 (HY-100351). This product is intended for research and analytical applications. BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.

GSK9311 (Standard) is the analytical standard of GSK9311 (HY-100729). This product is intended for research and analytical applications. GSK9311, a less active analogue of GSK6853, can be used as a negative control. GSK9311 inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.

GNE-781 (Standard) is the analytical standard of GNE-781 (HY-108696). This product is intended for research and analytical applications. GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC₅₀ of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC₅₀s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model.

Curcumin-d₃ (Diferuloylmethane-d₃ ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.

GNE-049 (Standard) is the analytical standard of GNE-049 (HY-108435). This product is intended for research and analytical applications. GNE-049 is a highly potent and selective CBP inhibitor with an IC₅₀ of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC₅₀s of 12 nM and 4200 nM, respectively.

XDM-CBP is a CBP/p300 inhibitor. XDM-CBP can be used in the study of malignant melanoma, breast cancer and leukemia.

CeMMEC1 (Standard) is the analytical standard of CeMMEC1 (HY-111445). This product is intended for research and analytical applications. CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC₅₀ of 0.9 μM for TAF1, and a K_d of 1.8 μM for TAF1 (2).