jq1

(+)-JQ-1 (JQ1) 是一种 BET 溴结构域抑制剂，抑制 BRD4(1 2) (IC50=77 33 nM)，具有特异性和可逆性。(+)-JQ-1 可以诱导细胞自噬，抑制细胞增殖。

JQ-1 (carboxylic acid) 是一种细胞渗透性 BRD4 抑制剂，对 BRD4(1) 和 BRD4(2) 的 IC50 分别为 77 和 33 nM。它是一种 (+)-JQ1 衍生物，可作为合成 PROTACs 的前体。

(R)-(-)-JQ1 Enantiomer 是 (+)-JQ1 的立体异构体。 (+)-JQ1 是一种 BET 溴结构域抑制剂，对BRD4(1 2)的IC50 为 77 和 33 nM。

(+)-JQ1 PA 是一种溴结构域和末端外 (BET) 抑制剂 JQ1 的衍生物，IC50 为 10.4 nM。

(+)-JQ1 maleimide是一种探针，由一个与BRD4配体JQ1通过PEG2连接器相连的含有活性的maleimide组成。它可用于COFFEE方法（COvalent Functionalization Followed by E3 Electroporation），在该方法中，(+)-JQ1 maleimide与VHL共价连接后通过电穿孔导入活细胞。E3连接酶在细胞内与BRD4形成复合物，引导其降解。

β-NF-JQ1是一种PROTAC，可将芳烃受体E3 （AhR E3） 连接酶招募到目标蛋白上。β-NF-JQ1使用β-NF 作为AhR 配体靶向含溴odomain（BRD）的蛋白，诱导AhR 和BRD 蛋白相互作用。β-NF-JQ1显示出与蛋白敲除活性相关的强大的抗癌活性 。

(+)-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.

ET-JQ1-OH 是一种等位基因特异性的 BET 抑制剂。

Biotinylated-JQ1 (Biotin-JQ1)为JQ1的一种生物素化衍生物，具有高亲和力地结合至BRD4溴域的能力。该化合物能有效抑制MM1.S多发性骨髓瘤细胞的增殖，其EC50值为0.4 μM。

JQ1-TCO (JQ1-trans-cycloctene) 是一种 BET 抑制剂 JQ1 的衍生物。JQ1-TCO 适用于点击化学，可作为体外和体内的分子探针。

NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1)是一款具有双功能的化合物，它通过特异性结合到细胞内特定亚细胞区室中的蛋白质，并以BRD4蛋白的核定位含溴结构域作为诱导，实现将胞浆中的货物输送至细胞核。

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

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].

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

JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222 是一种包含BRD4的配体与PROTAC接头的化合物，可用于合成PROTACBRD4 Degrader-29。

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 是一个有效的、异恶唑类的、BET 的广泛抑制剂，有着类似(+)-JQ1 的高选择性和强效作用，其对 BRD4(1) 的 KD 值为 5.43 nM。

VH032 thiol (VHL ligand 6) is a VHL ligand that interacts with pan-BET inhibitor JQ1 through a linker to create a PROTAC[1] compound.

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.

KB02-COOH is a synthetic fragment derived from ubiquitin E3 ligase ligand KB02, which possesses potential utility in the synthesis of PROTAC compounds. Notably, KB02-COOH can be employed in the generation of PROTAC constructs like KB02-JQ1 and KB02-SLF.

EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.1It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50= 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a cell-free assay when used at a concentration of 50 μM. EN219 (1 μM) also interacts with cysteine residues in the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60), also known as Hsp family D member 1 (HspD1), and histone H3.1 (HIST1H3A) in 231MFP human breast cancer cells in a proteomic profiling assay. It has been linked to the bromodomain and extra terminal domain (BET) inhibitor ligand (+)-JQ1 for use as a proteolysis-targeting chimera (PROTAC) to degrade bromodomain-containing protein 4 (BRD4) in 231MFP cells. 1.Luo, M., Spradlin, J.N., Boike, L., et al.Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product functionCell Chem. Biol.28(4)559-566(2021)

I-CBP112 hydrochloride 是含溴结构域转录因子的选择性抑制剂，靶向 CBP p300 溴结构域。在体内外，它以剂量依赖性方式显着降低 MLL-AF9(+) 急性髓细胞白血病细胞的白血病起始潜力，还增加 BET 溴结构域抑制剂 JQ1 以及阿霉素的细胞毒活性。

SJ46411-Br 作为一种CK1α分子胶 (Molecular Glue) 降解剂，该化合物在口服使用中显示出有效性。它能与CRL2KLHDC2结合，形成复合物以促进合作性同源选择性三元复合物的形成。此外，SJ46411-Br 可通过PROTAC linker 连接BET 配体 JQ1，进而制备相应的PROTACs。

β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) serves as an AhR E3 ligase ligand, forming chimeric molecules when connected to a protein ligand through a linker, resulting in PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1). These chimeric molecules recruit the AhR E3 ligase complex by incorporating AhR ligands. By inducing ubiquitination-mediated degradation, PROTACs effectively target and degrade cancer-promoting proteins [1].