PLX51107

PLX51107 is a bromodomain and extra terminal domain (BET) family protein inhibitor.¹ It binds to bromodomain 1 (BD1) in bromodomain-containing protein 2 (BRD2), BRD3, BRD4, and BRDT (K_ds = 1.6, 2.1, 1.7, and 5 nM, respectively), as well as BD2 (K_ds = 5.9, 6.2, 6.1, and 120 nM, respectively). It also binds to the bromodomains of CBP and p300 (K_ds = ~100 nM for both). PLX51107 (0.1-10 µM) inhibits CpG-induced proliferation of primary chronic lymphocytic leukemia (CLL) cells. In vivo, PLX51107 (0.5-10 mg/kg) inhibits Ba/F3 cell-induced splenomegaly in mice. It also reduces tumor volume and increases survival in YUMM3.3 and D4M3.A mouse syngeneic B-RAF^V600E mutant melanoma models.²

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1. Ozer, H.G., El-Gamal, D., Powell, B., et al. BRD4 profiling identifies critical chronic lymphocytic leukemia oncogenic circuits and reveals sensitivity to PLX51107, a novel structurally distinct BET Inhibitor. Cancer Discov. 8(4), 458-477 (2018).

2. Erkes, D.A., Field, C.O., Capparelli, C., et al. The next-generation BET inhibitor, PLX51107, delays melanoma growth in a CD8-mediated manner. Pigm. Cell Melanoma R. 32(5), 687-696 (2019).