Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for the bromodomain of BRD4. Biotinylated-JQ1 inhibits MM1.S multiple myeloma cells proliferation with the EC 50 of 0.4 μM. In Vitro Biotinylated-JQ1 (0.1 nM-100 μM; 72 hours) inhibits MM1.S cell proli...
(+)-JQ-1 is a potent, high Affinity selective BET bromodomain inhibitor (IC50 values are 17.7, 32.6, 76.9 and 12942 nM respectively For BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively; Kd values are 49, 59.5, 82, 90.1, 128 and 190 nM For BRD4...
Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for the bromodomain of BRD4. Biotinylated-JQ1 inhibits MM1.S multiple myeloma cells proliferation with the EC50 of 0.4 μM[1]. Biotinylated-JQ1 (0.1 nM-100 μM; 72 hours) inhibits MM1.S cell proliferation...
(Fig. 5.5A),37OTUB2,33NUDT7,33BRD4,38and MPC.39Often, target-based screening begins in an in vitro system, and ligands are optimized bygel-based ABPP. The optimized ligands are then assessed for affinity and selectivity; poor selectivity makes it challenging to detect, validate, and ...
Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML. Herrmann et al. Oncotarget. [Epub ahead of print], 2012;3:1588 Small-molecule inhibition of BRDT for male contraception. ...
关键词: (+)-JQ1, (+)-JQ1 supplier, BET, bromodomains, inhibitors, inhibits, potent, selective, high, affinity, NUT, midline, carcinomas, antitumor, male, contraceptive, BRD2, BRD3, BRD4, BRDT, sgc, autophagy, induces, activators, activates, induction, anti-inflammatory, coronavirus, SARS-...
The Bromodomain Extraterminal (BET) subfamily of chromatin readers is highly specific toward acetylated histone tails, with highest affinity for H4K12, and H4K5.8,9 This is interesting, as BRD2 and BRD4 preferentially bind H4K12ac.8,9 Moreover, H4K5ac and H4K12ac were specifically linked to...
BRD4 has been shown to regulate HPV and HSV infection, while JQ1 treatment reactivates HIV from latency33,34,35. In consideration of the significance of histone modifications in gene regulation, we tested whether JQ1 and structurally different BRD4 inhibitors had any effect on Ad infection and Ad...
(−)-JQ1 enantiomer has no appreciable affinity to BET bromodomains, whereas enantiomerically pure (+)-JQ1 binds to BRD4 bromodomains 1 and 2 with Kd values of ~ 50 and 90 nM, respectively. Peptide Sequence: N/A Appearance: Off-white solid Formulation: N/A CAS Number: 1268524-71-5 ...
Investigational New DrugsJung M, Philpott M, Muller S, Schulze J, Badock V, Eberspacher U, et al. Affinity map of bromodomain protein 4 (BRD4) interactions with the histone H4 tail and the small molecule inhibitor JQ1. J Biol Chem. 2014;289(13):9304–19. Central...