Potent and selective BRPF1 bromodomain inhibitor, with an IC50 of 80nM. PFI-4 exhibits >100-fold selectivity for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4. PFI-4 specifically binds to the bromodomain of BRPF1 (Kd = 13nM), inhibiting binding to tri-acetylated histone 4 (residues...

BET bromodomain inhibitor with Kd values of 160, 170, 380, 490, 830 and 850nM for BRD4(1), BRD2(1), BRD3(1), BRD3(2), BRD2(2) and BRD4(2), respectively. XD14 also inhibits BRDT(1), CBP, p300 and BRDT(2) with Kd values of 1.2, 1.6, 2.6 and 3.7µM, respectively. XD14 has shown to attenuate proliferation of HL-60...

XD14 is a bromodomain-containing protein (BRD) inhibitor. It binds to BRD2, -3, and -4 (Kds = 170, 380, and 160 nM) and inhibits the growth of HL-60 cells (GI50 = ~20 µM). XD14 (10 µM) also inhibits the growth of SR, K562, and MOLT-4 leukemia cells, as well as T47D breast, UO-31 renal, IGROV-1 ovarian, and KM12...

Description: XD14 is an inhibitor of BET bromodomain (Kd of 160 nM, 170 nM, 380 nM, 490 nM, 830 nM and 850 nM for BRD4(1), BRD2(1), BRD3(1), BRD3(2), BRD2(2) and BRD4(2), respectively). Target: Epigenetic Reader Domain. Smiles: CCN(CC)S(=O)(=O)c1ccc(O)c(NC(=O)c2[nH]c(C)c(C(C)=O)c2CC)c1. References: Daqiang P ,...