(+)jq1

(+)-JQ1 PA, a derivative of the Bromodomain and extra-terminal (BET) inhibitor JQ1, exhibits an IC50 of 10.4 nM.

(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.

(+)-JQ1 maleimide, featuring a cysteine-reactive maleimide linked to the BRD4 ligand, JQ1, via a PEG2 linker, serves as a probe suitable for the COFFEE method (COvalent Functionalization Followed by E3 Electroporation). This approach facilitates the covalent attachment of (+)-JQ1 maleimide to VHL, followed by electroporation into live cells, where the E3 ligase complexes with intracellular BRD4 to prompt its degradation.

(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1/2) with IC50 values of 77/33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

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

β-NF-JQ1 is a PROTAC that recruits aryl hydrocarbon receptor E3 (AhR E3) ligase to target proteins. Using β-NF as an AhR ligand, it targets bromodomain (BRD)-containing proteins and induces AhR and BRD protein interactions. β-NF-JQ1 exhibits potent anticancer activity associated with protein knockdown activity.

KB02-JQ1 is a potent and specific proteolysis targeting chimera (PROTAC) that specifically degrades BRD4, acting as a molecular glue. It does not degrade BRD2 or BRD3. The mechanism of action involves covalent modification of the E3 ligase DCAF16, thereby promoting BRD4 degradation. Importantly, KB02-JQ1 demonstrates enhanced stability and durability in facilitating protein degradation within biological systems. The compound forms a complex with the ubiquitin E3 ligase ligand KB02 through a linker, resulting in the formation of KB02-JQ1[1].

(+)-JQ1-OH is the primary metabolite of (+)-JQ1. (+)-JQ-1 (JQ1) is a potent, specific, and reversible inhibitor of BET bromodomain, with IC50 values of 77 nM for the first bromodomain and 33 nM for the second bromodomain (BRD4(1/2)). Additionally, (+)-JQ-1 stimulates autophagy (autophagy).

ZnPc-O3-JQ1 is a light-activated BRD4 degrader. Under light exposure, ZnPc-O3-JQ1 generates reactive oxygen species (ROS), leading to the degradation of BRD4. This degradation results in the downregulation of HIF-1α, effectively countering the tumor hypoxia-induced resistance to photodynamic therapy (PDT). ZnPc-O3-JQ1 exhibits both Type I and Type II PDT mechanisms. The structure of ZnPc-O3-JQ1 includes three components: a BRD4 ligand, a linker, and a photosensitizer.

Ad-JQ1 (Compound 16) is a Target Protein Ligand-Linker Conjugate incorporating a BRD4 ligand and a PROTAC linker capable of recruiting E3 ligase. It is utilized in the synthesis of PROTACβ-NF-JQ1.

ET-JQ1-OH (allele-specific BET inhibitor) is a chemical compound designed to inhibit bromodomain and extraterminal (BET) proteins in an allele-specific manner, impacting gene expression and associated pathological processes.

Calanolide B is one of a novel class of HIV-inhibiting coumarins from the tropical rainforest tree, Calophyllum lanigerum.

(+)-JQ-1 carboxylic acid is a potent bromodomain and extra terminal domain (BET) inhibitor. (+)-JQ-1 carboxylic has potential to be used as a precursor to synthesize PROTACs and other conjugates.

Biotinylated-JQ1 (Biotin-JQ1), a biotinylated derivative of JQ1, selectively binds to the BRD4 bromodomain with high affinity. It effectively inhibits the proliferation of MM1.S multiple myeloma cells, demonstrating an EC50 of 0.4 μM [1].

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].

NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1) is a bifunctional compound that facilitates the nuclear import of cytosolic cargoes by utilizing the nuclear-localized bromodomain-containing protein 4 (BRD4) as a carrier for co-import and subsequent nuclear entrapment [1].

(+)-JQ-1-aldehyde is the aldehyde derivative of (+)-JQ1, commonly used as a precursor for synthesizing PROTACs targeting the BET bromine domain[1].

JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222 incorporates a BRD4 ligand and a PROTAC linker, and is used in the synthesis of PROTAC BRD4 Degrader-29.

JQ-1 carboxylic acid-PEG3-C2-NH2 (hydrochloride) is an E3 ligase ligand-linker conjugate that is useful for synthesizing PRPTAC.

JQ-1-Azidopropylamine is a Target Protein Ligand-Linker Conjugate, composed of a BRD4 ligand and a PROTAC linker that recruits E3 ligase. It is used in the synthesis of PROTACJY-21.

AM-156 is a bio-active chemical.

Cacospongionolide B is isolated from the sponge Fasciospongia cavernosa. The marine sponge natural product cacospongionolide B (1) is one of a class of compounds bearing a g-hydroxybutenolide which are known to inhibit multiple forms of secratory phospholipase A2,1 enzymes believed to initiate a cascade of biological events leading to inflammation.

PNZ5, an isoxazole-based pan-BET inhibitor, demonstrates potent activity and high selectivity comparable to the established (+)-JQ1, exhibiting a dissociation constant (KD) of 5.43 nM for BRD4(1).

TD-428 is a highly specific degrader of BRD4(DC50 of 0.32 nM). TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation.