jq1-carboxylic-acid

Description: (+)-JQ1 carboxylic acid is the free carboxylic acid (COOH) form of (+)-JQ1 (tert-Butyl ester form-COOtBu). (+)-JQ1 is a potent and highly specific BET (Bromodomain and extra terminal domain) bromodomain inhibitor, with IC50 of 77 nM and 33 nM for BRD4(1/2) in enzymatic assays. (?)-JQ1 shows no significant interaction with any bromodomain. Besides, (?)-JQ1 enantiomer is comparatively inactive in nuclear protein in testis (NUT) midline carcinoma (NMC). (+)-JQ1 has high specificity for BET in that it only binds to bromodomains of the BET family, but not to any bromodomains of non-BET family. (+)-JQ1 has potential antineoplastic activity against various cancers such as MM (Multiple myeloma), pancreatic ductal adenocarcinoma and ovarian cancer etc. Its mechanism of action is to inhibit c-MYC and upregulate p21. (+)-JQ1 has been used as a chemical probe to investigate the role of BET bromodomains in the transcriptional regulation of oncogenesis.

References: Nature. 2010 Dec 23; 468(7327):1067-73; Cell. 2011 Sep 16; 146(6):904-17; Proc Natl Acad Sci U S A. 2011 Oct 4; 108(40):16669-74.

Related CAS#:1268524-71-5 (-)-JQ-1; 1268524-70-4 (+)-JQ1; 2115701-93-2 (+)-JQ1 PA