Drug intelligence / Profile preview

JQ1

Development stage
Preclinical
Lead developer
Dana-Farber Cancer Institute
Modality
Small Molecules
Administration
Intraperitoneal (in Mouse Studies)
01

Overview

JQ1 is a thienotriazolodiazepine and a potent inhibitor of the BET family of bromodomain proteins, including BRD2, BRD3, BRD4, and BRDT. It was developed by the James Bradner laboratory at Brigham and Women's Hospital and is used primarily in research settings due to its short half-life. JQ1 has shown efficacy in mouse models of cancer, particularly in NUT midline carcinoma, and has potential applications in treating other cancers, HIV infection, as a male contraceptive, and in slowing heart disease progression.

Other names
(+)-JQ1(+)-JQ-1(S)-(+)-tert-Butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate
02

Targets

PXR (Pregnane X receptor)BRDT (Bromodomain testis-specific protein)BRD4 (Bromodomain-containing protein 4)BRD2 (Bromodomain-containing protein 2)BRD3 (Bromodomain-containing protein 3)

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