(+)-JQ-1
JQ-1 is a triazolothienodiazepine compound that inhibits the BET bromodomain (BRD) family of proteins. Although it is a diazepine-like compound, JQ-1 exhibits no sedative or anxiolytic efficacy. JQ-1 was initially in development as a non-hormonal male contraceptive, inhibiting bromodomain testis-specific protein BRDT and chromatin remodeling during spermatogenesis, therefore preventing sperm production. This compound also activates latent HIV-1 in vitro and inhibits T cell proliferation through downregulation of T cell activation signals CD3, CD28, and CXCR4; JQ-1 is currently used as an experimental tool for examining mechanisms of HIV-1 latency. Additionally, JQ-1 exhibits anticancer chemotherapeutic activity in vitro and in vivo; through its inhibition of BRD4, JQ-1 suppresses Myc expression, IL-7R expression, and reduces JAK/STAT phosphorylation, inducing cell cycle arrest and altering survival in a variety of cell lines. Biological bromodomain binding activity comes primarily from (+)-JQ-1; the (-)-JQ-1 stereoisomer does not bind BET bromodomains.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18829260
| Cas No. |
1268524-70-4 |
|---|---|
| Purity |
≥99% |
| Formula |
C23H25ClN4O2S |
| Formula Wt. |
456.99 |
| Melting Point |
109.5°C |
| Appearance |
White Crystal Powder |
product targets : Motilin Receptor inhibitors
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Da Costa D, Agathanggelou A, Perry T, et al. BET inhibition as a single or combined therapeutic approach in primary paediatric B-precursor acute lymphoblastic leukaemia. Blood Cancer J. 2013 Jul 19;3:e126. PMID: 23872705.
Ott CJ, Kopp N, Bird L, et al. BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia. Blood. 2012 Oct 4;120(14):2843-52. PMID: 22904298.
Banerjee C, Archin N, Michaels D, et al. BET bromodomain inhibition as a novel strategy for reactivation of HIV-1. J Leukoc Biol. 2012 Dec;92(6):1147-54. PMID: 22802445.
Zuber J, Shi J, Wang E, et al. RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia. Nature. 2011 Aug 3;478(7370):524-8. PMID: 21814200.
Filippakopoulos P, Qi J, Picaud S, et al. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. PMID: 20871596.
