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.

Jaceosidin (Standard) is a reference standard for research and analysis in studies involving Jaceosidin. 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 Cdc2-cyclin B1 complex, followed by G2/M cell cycle arrest in endometrial cancer cells. Jaceosidin has immunosuppressive effect through inhibiting T cell proliferation and activation, which is closely associated with its potent down-regulation of the IFN-γ/STAT1/T-bet signaling pathway. The pharmacokinetics of Jaceosidin may be dramatically affected by polymorphic CYP1A2, UGT1A1, and UGT1A7 responsible for the metabolism of Jaceosidin or by the coadministration of relevant CYP1A2 or UGT inhibitors or inducers.