I-BET151
Antagonist of BRD4, BRD2, BRD3
Structure
In Cells
In Model Organisms
SERP ratings and comments
SERP Ratings
SERP Comments:
In a single-dose, mouse PK study (IP administration), I-BET-151 showed increased exposure and half-life compared to JQ1.
(last updated: 20 May 2016 )
SERP Ratings
SERP Comments:
Due to the low potency of I-BET151, I would not recommend it as a cellular probe. More potent probes for BRD4 exist (e.g., JQ1 and I-BET762). None of these are selective for BRD4 though; they inhibit all of the BET family proteins with equal potency.
(last updated: 20 May 2016 )
SERP Ratings
SERP Comments:
There are a number of well-characterized tool molecules available for the BRD2/3/4 family, and anyone seeking to use one of these probes is advised to consult the Chemical Probes Portal pages to view the latest molecules and data before selecting the appropriate probe. Across the probes listed, JQ1, PFI-1 as well as this I-BET151 are all broadly selective for the sub-family of BRD4-related bromodomains, with some evidence of cellular and in vivo activity. The relative levels of potency/activity are different across these assays. This molecule (like JQ1) is very well characterized, with wide selectivity building confidence that this probe will act on the BRD4-related bromodomains rather than on other targets. I-BET151 is less potent than other BET inhibitors such as JQ1, but it has better in vivo PK properties in mice.
(last updated: 27 Apr 2017 )