PF-CBP1

ITC is the label-free technique for determining K _D values, PF-CBP1 is against CBP (K _d =0.19 μM) and >105-fold selective over BRD4 (K _d >20 μM) by ITC.PF-CBP1 displays greater than 100-fold selectivity for the bromodomain of CBP over those of BRD4 and a panel of other proteins, it against BRD2-1,BRD3-1, BRD3-2,BRD4-1, BRD4-2, BRDT-1, TAF1-2, and TAF1L-2 with IC ₅₀ values of 1.24 μM, 1.38 μM, 4.22 μM, 1.54 μM, 9.75 μM, 2.44 μM, 3.39 μM and 7.29 μM, respectively.PF-CBP1 (3-10 μM; pretreatment 30 mins; 4 hours) moderately reduces LPS-induced IL-6 and IFN-b expression in the J774 cell at 10 μM. And it decreases IL-1b expression evidently at 3 μM.PF-CBP1 (100 nM-1000 nM;24 hours) significantly reduced RGS4 mRNA levels(49% reduction) relative to vehicle in cortical neuron cells.