jq-1

(+)-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)

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.

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.

(+)-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.

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].

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.

(+)-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-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.

SNIPER(BRD)-1 is a chemical compound composed of a derivative of the IAP antagonist LCL-161 and the BET inhibitor (+)-JQ-1, linked together. It promotes the degradation of BRD4 through the ubiquitin-proteasome pathway and effectively degrades cIAP1, cIAP2, and XIAP with IC50 values of 6.8 nM, 17 nM, and 49nM, respectively[1].

SJ46421, a PROTAC protein degrader derived from (+)-JQ-1, targets KLHDC2. It efficiently forms a stable ternary complex with KLHDC2, exhibiting an IC50 of 7.8 nM. Furthermore, SJ46421 promotes the polyubiquitination of the BD2 domain of BRD2, BRD3, or BRD4.

JQ dS-4 is a degrader of Brahma-related gene 1 (BRG1)/BRM/SMARCA4 (PROTAC®; DC50 range = 9 - 390 nM in glioma models and cell lines), featuring a BRG1 inhibitor connected through a linker to a cereblon (CRBN) E3 ligase ligand. It effectively degrades BRG1 completely over 48 and 72 hours in HSJD-DIPG007 and SU-DIPGXIIIP cells. Additionally, it lessens the viability of various cancer cell lines, including those of H3K27M glioma, prostate, thyroid, and salivary gland.

Me-SJ46411 is an E3 ubiquitin ligase ligand used in the synthesis of PROTAC molecules. For instance, when combined with the PROTAC linker Boc-Piperazine-OH and the target protein ligand (+)-JQ-1, Me-SJ46411 can be employed to create the selective BRD3 PROTAC degrader SJ46420.

DP-15 acts as a degrader of GSPT1 and BRD4, with DC50 values of 5.25 nM and 0.48 nM, respectively. This compound exhibits antiproliferative activity in AML and NHL cells, showing IC50 values in the nanomolar range, induces G1 phase cell cycle arrest, and triggers apoptosis in MOLM13 cells. Additionally, DP-15 demonstrates anti-leukemic properties in the MOLM-13 xenograft mouse model. [Pink: ligand for target protein JQ-1 carboxylic acid; Black: linker; Blue: ligand for E3 ligaseCereblonThalidomide-5-OH]

SJ44236 is a BET PROTAC degrader capable of degrading BRD2 (DC50 = 0.127 nM), BRD3, and BRD4. It shows cytotoxicity in MV4-11 and HD-MB03 cells with IC50 values of 0.12 nM and 0.92 nM, respectively. The compound downregulates c-Myc expression and upregulates p53 expression. In mice, SJ44236 demonstrates good oral bioavailability (45%). [Pink: ligand for target protein JQ-1 carboxylic acid; Black: linker; Blue: ligand for E3 ligaseCereblonE3ligaseLigand 54]

LO-3-61 is a JQ-1 analog featuring a truncated fumarylamide group, classified as a BRD4 degrader with PROTAC (protein degradation targeting chimera) properties. It promotes the degradation of both long and short BRD4 isoforms via a CUL4DCAF16-dependent pathway. In MDA-MB-231 cells, LO-3-61 exhibits selectivity in degrading BRD3 and BRD4.