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.

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 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.

(+)-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.

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]

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.

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]