TP-472

TP-472 is an inhibitor of bromodomain BRD9 (K_d = 33 nM; EC₅₀ = 320 nM in a NanoBRET assay). It has >30-fold selectivity over all other bromodomain family members with the exception of the highly homologous BRD7 bromodomain (K_d = 340 nM in an isothermal titration calorimetry (ITC) assay). See the Structural Genomic Consortium (SGC) website for more information.

TP-472 is a selective BRD9/7 inhibitor, with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7[1][2]. TP-472 induces apoptosis of melanoma cells[3].

BRD9: 33 nM (Kd); BRD7: 0.34 μM (Kd)

Store at -20°C

[1] Moustakim M, et al. Chemical probes and inhibitors of bromodomains outside the BET family. Medchemcomm. 2016 Dec 7;7(12):2246-2264. DOI:10.1039/c6md00373g
[2] Gatchalian J, et al. A non-canonical BRD9-containing BAF chromatin remodeling complex regulates naive pluripotency in mouse embryonic stem cells. Nat Commun. 2018 Dec 3;9(1):5139. DOI:10.1038/s41467-018-07528-9
[3] Lawrence David Mason, et al. The BRD9/7 Inhibitor TP-472 Blocks Melanoma Tumor Growth by Suppressing ECM-Mediated Oncogenic Signaling and Inducing Apoptosis. Cancers (Basel). 2021 Nov 3;13(21):5516. DOI:10.3390/cancers13215516