brpf1

TRIM24 BRPF1-IN-2 is a selective dual TRIM24 BRPF1 inhibitor with anticancer activity that inhibits proliferation, gene and protein expression, and colony formation of prostate cancer cells in a dose-dependent manner.

HDAC6 8 BRPF1-IN-1 is a dual inhibitor targeting HDAC6, HDAC8, and the bromodomain and PHD finger containing protein 1 (BRPF1). It exhibits inhibitory activity against HDAC1, HDAC6, and HDAC8 with IC50 values of 797 nM, 344 nM, and 908 nM, respectively, and inhibits BRPF1 with a Kd value of 175.2 nM. This compound is utilized in cancer research [1].

HDAC8 BRPF1-IN-1 (Compound 23a) is a dual inhibitor targeting human HDAC8 (IC50: 443 nM) and human BRPF1 (Kd: 67 nM), with low in vitro activity against HDAC1 and HDAC6.

BRPF1B TRIM24-IN-1 (compound 34) is a potent inhibitor of TRIM24, BRPF1, and BRPF2, with IC50 values of 0.43 μM, 0.34 μM, and 1.75 μM respectively. The dissociation constants (KD) for its binding with the bromodomains of TRIM24, BRPF1, and BRD1 are 222 nM, 137 nM, and 1130 nM respectively.

GSK-5959 is an effective, specific and cell permeable BRPF1 bromodomain inhibitor (IC50: ~80 nM). The selectivity of GSK-5959 for BRPF1 is >100-fold over a panel of 35 other bromodomains, including BRPF2 3 and BET family bromodomains.

GSK9311 inhibits BRPF bromodomain (pIC50: 6.0 and 4.3 for BRPF1 and BRPF2, respectively). GSK9311 is a less active analog of GSK6853. It can be used as a negative control.

GSK9311 hydrochloride, a less active analog of GSK6853, can be used as a negative control. GSK9311 hydrochloride inhibits BRPF bromodomain (pIC50s: 6.0 and 4.3 for BRPF1 and BRPF2).

NI-42 is a structurally orthogonal chemical probe for the BRPFs and is biased. It effective inhibitor of the BRD of the BRPFs (IC50s of BRPF1 2 3=7.9 48 260 nM; Kds of BRPF1 2 3=40 210 940 nM). It also has excellent selectivity over nonclass IV BRD protei

GSK6853 is a potent, soluble, cell-active, and highly selective inhibitor of the BRPF1 bromodomain.

BAY-299 is an effecitve inhibitor of the bromodomain and PHD finger family member BRPF2 and the TATA box binding protein-associated factors TAF1 and TAF1L with IC50s of 67 nM, 8 nM, and 106 nM, respectively.

IACS-9571 (trifluoroacetate) serves as an inhibitor of the bromodomain proteins TRIM24 and BRPF1, exhibiting an IC50 of 8 nM and a Kd of 31 nM against TRIM24, and a Kd of 14 nM against BRPF1.

IACS-9571 (ASIS-P040) hydrochloride is a potent, selective inhibitor of TRIM24 and BRPF1, with an IC50 of 8 nM for TRIM24, and dissociation constants (Kd) of 31 nM for TRIM24 and 14 nM for BRPF1.

NI-57 is an inhibitor of the bromodomain and plant homeodomain finger-containing (BRPF) family proteins, with IC50 values of 3.1 nM for BRPF1, 46 nM for BRPF2 (BRD1), and 140 nM for BRPF3.

IACS-9571 is a selective and potent inhibitor of TRIM24 and BRPF1, (IC50: 8 nM for TRIM24; Kds: 31 nM and 14 nM for TRIM24 and BRPF1).

PFI-4 is a potent and selective and cell-permeable BRPF1 bromodomain inhibitor.