Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T17311 |
(+)-JQ1 PA
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
(+)-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。 | |||
T10526 |
β-NF-JQ1
|
Others | Others |
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 。 | |||
T19618 |
(R)-(-)-JQ1 Enantiomer
(R)-(-)2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮杂环庚烷-6-基)乙酸叔丁酯 |
Epigenetic Reader Domain | Chromatin/Epigenetic |
(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。 | |||
T2110 |
(+)-JQ-1
JQ1 |
Epigenetic Reader Domain; Autophagy; Ligands for Target Protein for PROTAC | Autophagy; Chromatin/Epigenetic; PROTAC |
(+)-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。 | |||
T18060 |
KB02-JQ1
|
Others | Others |
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 link... | |||
T70702 |
JQ1-Acid HCl
|
||
(+)-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. | |||
T5443 |
JQ-1 (carboxylic acid)
JQ-1 carboxylic acid |
Epigenetic Reader Domain | Chromatin/Epigenetic |
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。 | |||
T81675 |
NICE-01
AP1867-PEG2-JQ1,AP-PEG2-JQ1 |
||
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。 | |||
T83929 |
(+)-JQ1 maleimide
|
||
(+)-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。 | |||
T70700 |
Calanolide B
|
||
Calanolide B is one of a novel class of HIV-inhibiting coumarins from the tropical rainforest tree, Calophyllum lanigerum. | |||
T74753 | JQ1-TCO | ||
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。 | |||
T83931 |
JQ1-FITC
|
||
JQ1-FITC是一种荧光BET溴结构域探针。它与BRD4(BD1)和BRD4(BD2)具有高亲和力绑定(KD,app值分别为6.5 nM和5.8 nM,使用GST标签的BRD4蛋白,通过CoraFluorTR-FRET实验测定;在荧光偏振实验中,对于BRD4(BD1)的值为58.7 nM)。激发和发射峰(λ)分别为495 nm和525 nm。 | |||
T74428 | Biotinylated-JQ1 | ||
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。 | |||
T62357 |
ET-JQ1-OH
|
||
ET-JQ1-OH 是一种等位基因特异性的 BET 抑制剂。 | |||
T4495 |
dBET1
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
dBET1 是一种由 BRD4 抑制剂 JQ1 与 NSC 527179 衍生物通过 linker 产生的 PROTAC,可诱导 BRD4 降解。它是由Cereblon 配体和BRD4配体相连的PROTAC,其EC50值为 430 nM。 | |||
T12513 |
PNZ5
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
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。 | |||
T4247 |
I-CBP112 hydrochloride
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
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。 | |||
T16312 |
NH2-PEG3
PROTAC Linker 35 |
Others | Others |
NH2-PEG3 (PROTAC Linker 35) is a polyethylene glycol (PEG) linker utilized in the synthesis of PROTAC (β-NF-JQ1)[1]. | |||
T13981 |
β-Naphthoflavone-CH2-Br
β-NF-CH2-Br |
Others | Others |
β-Naphthoflavone-CH2-Br is an arylhydrocarbon receptor (AhR) ligand. β-Naphthoflavone-CH2-Br used to synthesize the PROTAC β-NF-JQ1. | |||
T18600 |
VH032 thiol
VHL ligand 6 |
Others | Others |
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. | |||
T35412 | (+)-JQ-1-aldehyde | ||
(+)-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]. | |||
T75170 | BI01826025 | ||
BI01826025 (pArg-JQ1) 是BRDTbromodomain1 (BRDTBD1)PROTAC 降解剂。BI01826025 可用于检测 ClpC2 对 ClpC1P1P2 蛋白酶的调控作用。 | |||
T75169 | SRG-II-19F | ||
SRG-II-19F (dCym-JQ1) 是 BRDTbromodomain1 (BRDTBD1) 降解剂。SRG-II-19F 可用于检测 ClpC2 对 ClpC1P1P2 蛋白酶的调控作用。 | |||
T13105 | TD-428 | Epigenetic Reader Domain | Chromatin/Epigenetic |
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. | |||
T70593 |
GW-841819X
|
||
GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X displayed activity in vivo against NUT-midline carcinoma, multiple myeloma, mixed-lineage leukemia, and acute myeloid leukemia. Bromodomain and extra-terminal (BET) proteins belong to a class of proteins collectively called epigenetic readers". BET bromodomains have emerged as promising drug targets for treatment of cancers | |||
T36574 |
GW841819X
GW841819X |
||
GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X was a single enantiomer but of undefined chirality at the 4-position of the benzodiazepine ring3. GW841819X and JQ1 were recently discovered that bind to the acetyl-lysine binding pocket of BET bromodomains with Kd ranges from 50 to 370 nM [1]. GW841819X bounded to both the individual BD1 and BD2 domains with affinities of 46 and 52.5 nM, respectively. GW841819X-Brd3 interaction was estimated to be around 70... | |||
T17363 |
β-Naphthoflavone-CH2-OH
β-NF-CH2-OH |
Others | Others |
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]. | |||
T41198 |
BRD PHOTAC-I-3
|
||
BRD PHOTAC-I-3 is a photoswitchable BET bromodomain degrader (PHOTAC, PHOtochemically TArgeting Chimera). BRD PHOTAC-I-3 comprises a ligand for an E3 ligase, a photoswitch, and the BET bromodomain targeting ligand (+)-JQ1. Exhibits cytotoxicity and degrades BRD4, BRD3 and to a lesser extent BRD2 in lymphoblast cells upon irradiation with 390 nm light, but not in the dark. | |||
T39923 |
KB02-COOH
KB02-COOH |
||
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. | |||
T36800 |
EN219
|
||
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 hum... |