bet-in-2

BET-IN-2 is a BET inhibitor with an IC50 of 52 nM for BRD4-BD1.

BET-IN-27 (compound 6C) is an orally active BET inhibitor with IC50 values of 3.3 nM (BRD4-BD2), 3.4 nM (BRD4-BD1), 4.1 nM (BRD2-BD1), 20.4 nM (BRD3-BD1), and 42.0 nM (BRDT-BD1). It also exhibits antiproliferative activity.

BET-IN-28 (Compound 44) is a potent inhibitor of bromodomain and extra-terminal domain (BET) proteins, exhibiting an IC50 value of 4.47 nM for BRD4-BD1. It obstructs the interaction between BET proteins and the N-acetylated lysine residues on histone tails, leading to the downregulation of specific gene expression. BET-IN-28 is applicable in research related to hematologic malignancies and solid tumors.

BET-IN-21 (compound 16) is a BET (Bromo and Extra-Terminal domain) inhibitor capable of penetrating the blood-brain barrier, with a Ki value of 230 nM. It suppresses microglial activation and demonstrates therapeutic effects in mice with experimental autoimmune encephalomyelitis.

BET-IN-26 (compound 13a) is a potent, selective, and orally active BD1 inhibitor, exhibiting IC50 values of 0.0055 µM for BD1 and 9.0 µM for BD2. It effectively reduces serum IL-6 and MCP-1 levels induced by LPS.

BET-IN-25 (compound 7) is an orally bioactive inhibitor targeting the bromodomains BD1 and BD2, with IC50 values of 0.18 μM and 9.2 μM, respectively.

BET-IN-20 (compound 10), a BRD4 BD1 inhibitor (IC 50 =1.9 nM), exhibits significant anticancer properties. It promotes apoptosis in acute myeloid leukemia (AML) cells and arrests the cell cycle in the G0/G1 phase. Additionally, BET-IN-20 inhibits both c-Myc and CDK6, and enhances PARP cleavage [1].

BET-IN-23 (Compound 23) is a BD2-selective BET inhibitor with an IC50 of 2.9 nM. It exhibits anticancer activity by significantly inhibiting the proliferation of acute myeloid leukemia (AML) cell lines, inducing G0/G1 arrest, and apoptosis in vitro [1].

CF53 is a highly potent, selective, and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM, and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, being very selective over non-BET bromodomain-containing proteins. CF53 exhibits potent anti-tumor activity both in vitro and in vivo.

(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is utilized in the synthesis of ARV-771, a potent BET protein degrader. It selectively degrades BET protein in castration-resistant cells with a DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, it serves as the VHL ligand from (S,R,S)-AHPC for recruiting von Hippel-Lindau (VHL) protein.

(S,R,S)-AHPC-Me dihydrochloride, also known as VHL ligand 2 dihydrochloride, is a chemical compound used in the synthesis of ARV-771. ARV-771 is a BET PROTAC degrader that relies on von Hippel-Landau (VHL) E3 ligase and exhibits potent degradation of BET proteins in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM. This compound acts as the VHL ligand, specifically the (S,R,S)-AHPC-based VHL ligand, facilitating the recruitment of von Hippel-Lindau (VHL) protein.

(R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1, a BET bromodomain inhibitor, which acts on BRD4(1/2) with IC50 values of 77 nM and 33 nM in a cell-free assay.

NB512 (compound 39a) is a dual inhibitor targeting both BET and HDAC, exhibiting high affinity for the BRD4 bromodomain and HDAC1/2, with EC50 values ranging from 100 to 400 nM. It demonstrates antiproliferative activity in cancer cell lines PaTu8988T and NMC.

Progranulin modulator-2 (compound 18A) is a novel bromodomain and extra-terminal domain (BET) inhibitor. By targeting BET protein family members, Progranulin modulator-2 enhances PGRN expression. It is applicable for studying the role of BET proteins in neurodevelopment, neural plasticity, and neurodegeneration.

AZD5153 6-Hydroxy-2-naphthoic acid (AZD5153) is a potent triazolopyridazine-based Bromodomain (BRD4) and Extraterminal (BET) inhibitor utilized in cancer treatments.

TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 μM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 μM) and for HDAC1 over HDAC2 (IC50= 2.5 μM). TW9 (50 nM) induces apoptosis in, and inhibits proliferation of, MIA PaCa-2 pancreatic cancer cells. It induces cell cycle arrest at the G1phase in HPAC pancreatic cancer cells when used at a concentration of 2 μM. TW9 acts synergistically with gemcitabine to reduce the viability of HPAC cells. 1.Zhang, X., Zegar, T., Weiser, T., et al.Characterization of a dual BET/HDAC inhibitor for treatment of pancreatic ductal adenocarcinomaInt. J. Cancer147(10)2847-2861(2020)

Glucosamine 6-sulfate (GlcN6S) is a glucosamine derivative exhibiting anti-inflammatory effects in experimental autoimmune encephalomyelitis (EAE). It inhibits gene expression of IL-12, T-bet, and IFN-γ, suppresses Th1 CD4 T cell differentiation, and may be utilised in multiple sclerosis (MS) research.

Jaceosidin has anti-oxidative activity. Jaceosidin has anti-inflammatory activity, also a microglial inhibitor with anti-neuroinflammation activity. aceosidin has anticancer activity, modulates the ERK/ATM/Chk1/2 pathway, leading to inactivation of the Cd

Ethyl Caffeate (ETHYL 3,4-DIHYDROXYCINNAMATE) suppressed the differentiation of naive CD4+ T cells into Th1 in vitro. Furthermore, Ethyl Caffeate intensely blocked the transcriptional expression in interferon-γ-related signaling, including IFN-γ, T-bet, STAT1, and STAT4.

JQ1-TCO (JQ1-trans-cyclooctene), a derivative of the BET inhibitor JQ1, is designed for click chemistry applications, enabling its use as molecular probes both in vitro and in vivo [1] [2].

(S,R,S)-AHPC-Me (E3 ligase Ligand 1A) (VHL ligand 2) is an (S,R,S)-AHPC-based VHL ligand used to recruit the von Hippel-Lindau (VHL) protein. It is utilized in the synthesis of ARV-771, a VHL E3 ligase-based BET PROTAC degrader that effectively degrades BET proteins in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.