jq 1 (carboxylic acid)

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

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)-amine-PEG8-cyanogen is a Target Protein Ligand-Linker Conjugate, comprising a BRD4 ligand and a PROTAC linker, which recruits E3 ligase. This compound is utilized for the synthesis of PROTAC BET Degrader-14.

JQ-1 (carboxylic acid)-NH-C8-COOH is a synthetic target protein ligand-linker conjugate used in the synthesis of JQ1-S(GlcNAc)Cq. JQ1-S(GlcNAc)Cq is a potent enzyme-activated glycosylation (Sugar-CoatedPROTAC) bifunctional degrader with antitumor activity.

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]

JQ-1 (carboxylic acid)-amine-PEG8-cyanogen is a PEG-based PROTAC linker used in the synthesis of PROTACs.

(+)-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.