BRD9-PROTAC-E5

BRD9-PROTAC-E5 : Degrader (PROTAC) of BRD9

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe BRD9-PROTAC-E5 is in the process of SERP review.

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Information

BRD9

Degrader (PROTAC)

up to 10 nM

In Vitro Validations

No in Vitro Validations

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): PROTAC E5 did not induce the degradation of BRD4 and BRD7 in MV4-11 cells up to 100 nM. E5 had excellent selectivity for neo-substrate recruitment with no GSPT1 degradation. Degradation activity toward IKZF1 was compared to the degradation of BRD9, E5 showed only moderately deviating IKZF1 degradation activity. In proteomics, a total of 4849 proteins were examined. Quantitative proteomic experiment revealed that the homologous Bromodomain proteins, including BET family proteins, were not significantly affected. Similar results were observed in Western Blot. CHEK2, KHDC4, CELF1, and TTK also showed notable downregulation and it was found that the changes in these proteins might result from signaling pathway alterations caused by the degradation of BRD9.

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

In some cell lines, the compound is less effective (SU-DHL-6 (374nM) and U937 (1um))

(last updated: 30 Jul 2024 )