Order now on opnMe: BI-7190, a BPTF bromodomain inhibitor to explore epigenetics
08 August 2022
The BPTF (Bromodomain PHD Finger Transcription Factor) protein is a histone-binding component of the NURF complex (nucleosome-remodeling factor) and plays an important role in chromatin remodeling. On opnMe, we are delighted to share a selective bromodomain inhibitor BI-7190 for scientists all over the world to study BPTF’s roles in epigenetics and disease biology.
BI-7190 was discovered by screening selected analogs of the BRD9 inhibitor BI-9564. It was shown to bind with high affinity to the BPTF bromodomain, with more than a 19-fold window towards BRD9. BI-7190 is a potent epigenetic inhibitor which can be used to study the impact of BPTF bromodomain inhibition.
Importantly, the combination of potency, selectivity, and good ADME parameters makes BI-7190 a good probe to study the impact of inhibiting the epigenetic reader function of BPTF in vitro and in vivo, a unique feature compared to other BPTF probes that were already available.
As a researcher, you are now able to obtain BI-7190 and BI-9564 along with their negative controls completely free of charge. You will own all results you will generate with the molecules and may use them for your own publications.
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About BI-7190:
BI-7190 is a probe to study the impact of BPTF bromodomain inhibition in vitro and in vivo. It binds with high affinity to the bromodomain of BPTF (58nM nanoBRET) and displays good cellular potency and shows high selectivity at 10 μM on a panel of 44 receptors and 38 kinases (no inhibition). BI-4827 is an inactive analog of BI-7190 and can be used as negative control for in vitro experiments. The negative control BI-4827 shows high selectivity hitting 0/44 targets inhibition with more than 50% @10 μM.
About BI-9564:
BI-9564 inhibits the human BRD9 with an KD (BRD9, ITC) of 14 nM, displays good cellular potency and an excellent selectivity versus most BET family members. It binds with high affinity to BRD9 and with lower affinity to closely related BRD7 KD (BRD7, ITC) = 239 nM. BI-9464 is completely negative on BET family members in the AlphaScreen (>100 µM). BI-6354 is available as an in vitro negative control. It shows only very weak potency on BRD9 and BRD7 and no potency on BRD4.
About opnMe:
opnMe.com, the new open innovation portal of Boehringer Ingelheim, aims to accelerate research initiatives to enable new insights of disease biology in areas of high unmet medical need by sharing well-characterized molecules and offer collaborations for science. In the spirit of collaboration, our molecules are provided to the scientific community to help unlock and fulfill their full potential. These molecules are either freely available as “Molecules to Order” or applied via scientific research submissions via our “Molecules for Collaboration” calls. As part of our third pillar, our “opn2EXPERTS” program, we also enlist scientific advice on key biologic issues to fuel further drug discovery and deliver novel solutions that benefit unmet patient needs, such as our latest call on identifying ligands for GPR151.